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	Agonist activity at FFA1 (unknown origin)	F	7.89	pEC50	13	nM	EC50	Eur J Med Chem (2023) 245: 114883-114883 [PMID:36343410]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]