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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

AMG-837	395	None	35	Human	Binding	EC50	=	13.00	7.89	-	3	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.bmcl.2015.11.050
AMG-837	395	None	35	Human	Binding	Kd	=	1.90	8.72	-	3	Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
AMG-837	395	None	35	Human	Binding	EC50	=	11.00	7.96	-	3	Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
AMG-837	395	None	35	Human	Binding	Ki	=	2.20	8.66	-	3	Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
AMG-837	395	None	35	Human	Binding	EC50	=	2.20	8.66	-	3	Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acsmedchemlett.6b00331
AMG-837	395	None	35	Human	Binding	EC50	=	23.00	7.64	-	3	Agonist activity at FFA1 receptor (unknown origin)	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.bmc.2016.09.004
AMG-837	395	None	35	Human	Binding	Ki	=	41.69	7.38	-	3	Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00202
AMG-837	395	None	35	Human	Binding	EC50	=	154.88	6.81	-	3	Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00202
AMG-837	395	None	35	Human	Binding	EC50	=	80.00	7.10	-	3	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.bmcl.2015.11.050
AMG-837	395	None	35	Human	Binding	EC50	=	8800.00	5.06	-	3	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.bmcl.2015.11.050
AMG-837	395	None	35	Human	Binding	EC50	=	104.00	6.98	-	3	Agonist activity at human GPR40 expressed in CHO cells by aequorin assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/ml400501x
AMG-837	395	None	35	Human	Binding	EC50	=	60.00	7.22	-	3	Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/ml300427u
AMG-837	395	None	35	Mouse	Binding	EC50	=	1.50	8.82	-	3	Agonist activity at Prolink-tagged mouse GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
AMG-837	395	None	35	Rat	Binding	EC50	=	3.20	8.49	-	3	Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
BENZYLOXYPHENYLPROPANOIC ACID	58844	None	46	Human	Binding	EC50	=	549.54	6.26	-	2	Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins by BRET assay	ChEMBL	256.1	6	1	2	3.28	O=C(O)CCc1ccc(OCc2ccccc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00202
BENZYLOXYPHENYLPROPANOIC ACID	58844	None	46	Human	Binding	Ki	=	13803.84	4.86	-	2	Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)propanoic acid from N-terminal NLUC-tagged FFA1 receptor (unknown origin) expressed in human Flp-In T-REX-293 cell membrane coexpressing mGluR5 incubated for 1 hr by equilibrium BRET assay	ChEMBL	256.1	6	1	2	3.28	O=C(O)CCc1ccc(OCc2ccccc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00202
CHEMBL1170012	10602	None	37	Human	Binding	EC50	=	48977.88	4.31	-	2	Agonist activity at human FFA1 receptor expressed in CHO-K1 cells assessed as increase in dynamic mass redistribution response by DMR assay	ChEMBL	315.1	3	1	2	3.81	Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1	https://dx.doi.org/10.1016/j.bmcl.2020.127650
CHEMBL1688457	58849	None	0	Human	Binding	EC50	=	75.00	7.12	-	2	Agonist activity at GPR40 (unknown origin)	ChEMBL	332.1	7	1	2	4.95	O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115263
CHEMBL1688473	58866	None	0	Human	Binding	Ki	=	32.00	7.50	1	3	Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from human GPR40 expressed in CHO membranes after 90 mins by liquid scintillation counting in presence of 0.2 % BSA	ChEMBL	378.2	7	1	2	5.71	Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1	https://dx.doi.org/10.1021/ml1000855
CHEMBL1688473	58866	None	0	Human	Binding	Ki	=	32.00	7.50	1	3	Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA	ChEMBL	378.2	7	1	2	5.71	Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1	https://dx.doi.org/10.1021/jm2016123

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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

α-linolenic acid	363	None	48	Human	Functional	pEC50	=	-	5.15	1	3	Unclassified	Guide to Pharmacology	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://pubmed.ncbi.nlm.nih.gov/12496284
α-linolenic acid	363	None	48	Human	Functional	pEC50	=	-	5.15	1	3	Unclassified	Guide to Pharmacology	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://pubmed.ncbi.nlm.nih.gov/12565875
α-linolenic acid	363	None	48	Human	Functional	pEC50	=	-	5.15	1	3	Unclassified	Guide to Pharmacology	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://pubmed.ncbi.nlm.nih.gov/12629551
α-linolenic acid	363	None	48	Human	Functional	pEC50	=	5.52	8.26	1	3	Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay	Drug Central	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	-
α-linolenic acid	363	None	48	Human	Functional	EC50	=	11090.00	4.96	1	3	Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay	ChEMBL	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://dx.doi.org/10.1016/j.ejmech.2018.08.075
α-linolenic acid	363	None	48	Human	Functional	EC50	=	3000.00	5.52	1	3	Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay	ChEMBL	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.5b01962
α-linolenic acid	363	None	48	Human	Functional	EC50	=	3162.28	5.50	1	3	Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay	ChEMBL	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.5b01962
α-linolenic acid	363	None	48	Human	Functional	EC50	=	2884.03	5.54	1	3	Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay	ChEMBL	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://dx.doi.org/10.1021/jm300215x
α-linolenic acid	363	None	48	Human	Functional	EC50	=	5200.00	5.28	1	3	Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay	ChEMBL	278.2	13	1	1	5.66	CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O	https://dx.doi.org/10.1021/jm800970b
2-hydroxylauric acid	66	None	35	Human	Functional	EC50	=	6760.83	5.17	1	2	Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human FFA1 receptor expressed in HEK293T cells assessed as induction of beta-arrestin-2 recruitment after 15 mins by BRET assay	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCCC(O)C(=O)O	https://dx.doi.org/10.1039/C7MD00130D
AMG-837	395	None	35	Human	Functional	pEC50	=	-	8.50	-8	3	Unclassified	Guide to Pharmacology	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://pubmed.ncbi.nlm.nih.gov/22859723
AMG-837	395	None	35	Human	Functional	EC50	=	13.00	7.89	-8	3	Agonist activity at FFA1 (unknown origin)	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.ejmech.2018.09.071
AMG-837	395	None	35	Human	Functional	EC50	=	13.00	7.89	-8	3	Agonist activity at FFA1 (unknown origin)	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.ejmech.2022.114883
AMG-837	395	None	35	Human	Functional	EC50	=	1.30	8.89	-8	3	Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
AMG-837	395	None	35	Human	Functional	EC50	=	15.00	7.82	-8	3	Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in intracellular calcium level measured over 3 mins by calcium 4 dye based FLIPR assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00892
AMG-837	395	None	35	Human	Functional	EC50	=	13.00	7.89	-8	3	Agonist activity at GPR40 (unknown origin) by calcium flux assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1016/j.bmcl.2016.10.074
AMG-837	395	None	35	Human	Functional	EC50	=	169.82	6.77	-8	3	Agonist activity at FFA1 receptor (unknown origin) expressed in human 132N1 cells measured for 90 secs by Fura-2 AM dye based calcium mobilization assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00202
AMG-837	395	None	35	Human	Functional	EC50	=	41.00	7.39	-8	3	Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/ml400501x
AMG-837	395	None	35	Human	Functional	EC50	=	60.00	7.22	-8	3	Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/ml300133f
AMG-837	395	None	35	Human	Functional	EC50	=	100.00	7.00	-8	3	Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry	ChEMBL	438.1	7	1	2	6.53	CC#C[C@@H](CC(=O)O)c1ccc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)cc1	https://dx.doi.org/10.1021/jm2005699

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Ligand source activities (1 row/activity)