ChEMBL ligand: CHEMBL1829173 (AMG-837)
FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842] FFA1 receptor/Free fatty acid receptor 1 in Mouse [ChEMBL: CHEMBL5411] [GtoPdb: 225] [UniProtKB: Q76JU9] FFA1 receptor/Free fatty acid receptor 1 in Rat [ChEMBL: CHEMBL1795180] [GtoPdb: 225] [UniProtKB: Q8K3T4] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL	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	B	8.72	pKd	1.9	nM	Kd	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
ChEMBL	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	B	7.38	pKi	41.69	nM	Ki	J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL	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	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
ChEMBL	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum	B	5.06	pEC50	8800	nM	EC50	Bioorg Med Chem Lett (2016) 26: 15-20 [PMID:26620255]
ChEMBL	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	F	6.77	pEC50	169.82	nM	EC50	J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL	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	B	6.81	pEC50	154.88	nM	EC50	J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL	Agonist activity at human GPR40 expressed in CHO cells by aequorin assay	B	6.98	pEC50	104	nM	EC50	ACS Med Chem Lett (2014) 5: 517-521 [PMID:24900872]
ChEMBL	Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry	F	7	pEC50	100	nM	EC50	J Med Chem (2011) 54: 6691-6703 [PMID:21854074]
ChEMBL	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	B	7.1	pEC50	80	nM	EC50	Bioorg Med Chem Lett (2016) 26: 15-20 [PMID:26620255]
ChEMBL	Agonist activity at human FFA1 receptor expressed in CHO cell membranes after 4 hrs by aequorin bioluminescence assay	B	7.22	pEC50	60	nM	EC50	ACS Med Chem Lett (2013) 4: 551-555 [PMID:24900707]
ChEMBL	Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 0.1 % human serum	F	7.22	pEC50	60	nM	EC50	ACS Med Chem Lett (2012) 3: 726-730 [PMID:24900539]
ChEMBL	Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay	F	7.39	pEC50	41	nM	EC50	ACS Med Chem Lett (2014) 5: 517-521 [PMID:24900872]
ChEMBL	Agonist activity at FFA1 receptor (unknown origin)	B	7.64	pEC50	23	nM	EC50	Bioorg Med Chem (2016) 24: 5481-5494 [PMID:27647366]
ChEMBL	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	F	7.82	pEC50	15	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
ChEMBL	Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis	B	7.89	pEC50	13	nM	EC50	Bioorg Med Chem Lett (2016) 26: 15-20 [PMID:26620255]
ChEMBL	Agonist activity at GPR40 (unknown origin) by calcium flux assay	F	7.89	pEC50	13	nM	EC50	Bioorg Med Chem Lett (2016) 26: 5603-5612 [PMID:27825762]
ChEMBL	Agonist activity at FFA1 (unknown origin)	F	7.89	pEC50	13	nM	EC50	Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL	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	B	7.96	pEC50	11	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
GtoPdb	-	-	8.5	pEC50	-	-	-	Mol Pharmacol (2012) 82: 843-59 [PMID:22859723]
ChEMBL	Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay	B	8.66	pEC50	2.2	nM	EC50	ACS Med Chem Lett (2016) 7: 1134-1138 [PMID:27994752]
ChEMBL	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	F	8.89	pEC50	1.3	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
FFA1 receptor/Free fatty acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5411] [GtoPdb: 225] [UniProtKB: Q76JU9]
ChEMBL	Agonist activity at mouse GPR40	F	7.89	pEC50	13	nM	EC50	Bioorg Med Chem Lett (2012) 22: 1267-1270 [PMID:22217876]
ChEMBL	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	B	8.82	pEC50	1.5	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
FFA1 receptor/Free fatty acid receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795180] [GtoPdb: 225] [UniProtKB: Q8K3T4]
ChEMBL	Agonist activity at rat GPR40	F	7.64	pEC50	23	nM	EC50	Bioorg Med Chem Lett (2012) 22: 1267-1270 [PMID:22217876]
ChEMBL	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	B	8.49	pEC50	3.2	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]