ChEMBL ligand: CHEMBL1829174 (Fasiglifam, Fasiglifam hemihydrate, Fasiglifam hydrate, TAK875, TAK-875, Tak-875 anhydrous)
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] There should be some charts here, you may need to enable JavaScript!
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!
FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] There should be some charts here, you may need to enable JavaScript!
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6] 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
Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
ChEMBL	Inhibition of NTCP in human hepatocytes	B	5.7	pIC50	2000	nM	IC50	Bioorg Med Chem Lett (2019) 29: 126623-126623 [PMID:31439379]
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
ChEMBL	Binding affinity to human GPR40 expressed in CHO cells by LC-MS analysis	B	7.92	pKd	11.9	nM	Kd	J Med Chem (2020) 63: 10352-10379 [PMID:32900194]
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	8.35	pKd	4.5	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	7.54	pKi	28.84	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	8.11	pKi	7.7	nM	Ki	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
ChEMBL	Transactivation of human GPR40 expressed in HEK293 cells after 24 hrs by Elk-Gal4 luciferase reporter assay	F	5.29	pEC50	5100	nM	EC50	Bioorg Med Chem Lett (2018) 28: 3050-3056 [PMID:30097366]
ChEMBL	Agonist activity at human GPR40 expressed in CHO cells incubated for 60 mins by FLIPR based Ca2+ mobilization assay	F	6	pEC50	>1000	nM	EC50	J Med Chem (2020) 63: 10352-10379 [PMID:32900194]
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	6.8	pEC50	160	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
ChEMBL	Agonist activity at human FFA1 receptor expressed in HEK293 cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based assay	F	7.1	pEC50	80	nM	EC50	Bioorg Med Chem Lett (2019) 29: 848-852 [PMID:30685095]
ChEMBL	Agonist activity at human GPR40 expressed in human HEK293 cells assessed as increase in intracellular calcium flux after 10 mins by fluorescence assay	F	7.1	pEC50	80	nM	EC50	Bioorg Med Chem (2018) 26: 5780-5791 [PMID:30392954]
GtoPdb	-	-	7.1	pEC50	-	-	-	J Pharmacol Exp Ther (2011) 339: 228-37 [PMID:21752941]; Nature (2014) 513: 124-7 [PMID:25043059]; Diabetes Obes Metab (2015) 17: 675-81 [PMID:25787200]; ACS Med Chem Lett (2010) 1: 290-4 [PMID:24900210]
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	7.24	pEC50	57.54	nM	EC50	J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL	Agonist activity at GPR40 (unknown origin)	B	7.28	pEC50	53	nM	EC50	Bioorg Med Chem (2020) 28: 115574-115574 [PMID:32546302]
ChEMBL	Agonist activity at human FFA1 receptor expressed in CHO cells by Fluo 4-AM dye based FLIPR assay	B	7.35	pEC50	45	nM	EC50	Eur J Med Chem (2019) 164: 352-365 [PMID:30605833]
ChEMBL	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay	F	7.35	pEC50	45	nM	EC50	Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL	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	F	7.41	pEC50	39	nM	EC50	Eur J Med Chem (2018) 158: 123-133 [PMID:30212763]
ChEMBL	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ concentration by Fluo-4 AM based fluorescence assay	F	7.41	pEC50	38.6	nM	EC50	Bioorg Med Chem (2015) 23: 132-140 [PMID:25481394]
ChEMBL	Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay	F	7.43	pEC50	37.1	nM	EC50	Eur J Med Chem (2019) 179: 608-622 [PMID:31279294]
ChEMBL	Agonist activity at human FFAR1 expressed in CHO cells assessed as increase in intracellular calcium level by Fluo 4-AM dye-based FLIPR assay	F	7.47	pEC50	33.6	nM	EC50	Bioorg Med Chem (2017) 25: 6647-6652 [PMID:29100735]
ChEMBL	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium levels measured for 90 secs by Fluo 4-AM dye based FLIPR assay	F	7.49	pEC50	32.5	nM	EC50	Bioorg Med Chem (2018) 26: 4560-4566 [PMID:30082106]
ChEMBL	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo-4 dye based FLIPR assay	F	7.5	pEC50	31.8	nM	EC50	Bioorg Med Chem (2018) 26: 703-711 [PMID:29291938]
ChEMBL	Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	F	7.51	pEC50	31	nM	EC50	ACS Med Chem Lett (2019) 10: 16-21 [PMID:30655940]
ChEMBL	Agonist activity at human FFA1 expressed in CHO cells assessed as intracellular Ca2+ level measured for 90 secs by Fluo-4 AM-based FLIPR assay	F	7.53	pEC50	29.6	nM	EC50	Bioorg Med Chem (2016) 24: 1981-1987 [PMID:27020683]
ChEMBL	Agonist activity at human FFA1 receptor expressed in CHO cells assessed as increase in intracellular calcium flux by FLIPR assay	F	7.53	pEC50	29.6	nM	EC50	Bioorg Med Chem (2015) 23: 7158-7164 [PMID:26482570]
ChEMBL	Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method	F	7.53	pEC50	29.6	nM	EC50	Bioorg Med Chem (2015) 23: 6666-6672 [PMID:26420383]
ChEMBL	Agonist activity at human GPR40 expressed in CHO cells by FLIPR calcium flux assay	F	7.56	pEC50	27.5	nM	EC50	Eur J Med Chem (2016) 116: 46-58 [PMID:27054485]
ChEMBL	Agonist activity at human GPR40 expressed in CHO cells assessed as increase in intracellular Ca2+ flux by Fluo 4-AM dye based assay	F	7.57	pEC50	27	nM	EC50	J Med Chem (2017) 60: 2697-2717 [PMID:28277660]
ChEMBL	Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA	F	7.8	pEC50	16	nM	EC50	J Med Chem (2012) 55: 3960-3974 [PMID:22490067]
ChEMBL	Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry	F	7.85	pEC50	14.13	nM	EC50	J Med Chem (2011) 54: 6691-6703 [PMID:21854074]
ChEMBL	Agonist activity at FFA1 (unknown origin)	F	7.85	pEC50	14	nM	EC50	Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL	Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay	F	7.85	pEC50	14	nM	EC50	ACS Med Chem Lett (2017) 8: 1336-1340 [PMID:29259758]
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	7.92	pEC50	12	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
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	8.03	pEC50	9.33	nM	EC50	J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
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	8.72	pEC50	1.9	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	9.46	pEC50	0.35	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 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	8.07	pEC50	8.6	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 GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA	B	4.57	pEC50	27000	nM	EC50	ACS Med Chem Lett (2016) 7: 1134-1138 [PMID:27994752]
ChEMBL	Agonist activity at rat GPR40 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by Fluo-8 dye based FLIPR assay	F	7.41	pEC50	39	nM	EC50	ACS Med Chem Lett (2019) 10: 16-21 [PMID:30655940]
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	7.44	pEC50	36	nM	EC50	J Med Chem (2016) 59: 10891-10916 [PMID:27749056]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL	Agonist activity at human FFAR4 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by luminescence assay	F	5	pEC50	>10000	nM	EC50	Bioorg Med Chem (2017) 25: 6647-6652 [PMID:29100735]
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
ChEMBL	Inhibition of human OATP1BA	B	5.64	pIC50	2280	nM	IC50	Bioorg Med Chem (2018) 26: 5780-5791 [PMID:30392954]

ChEMBL data shown on this page come from version 32:

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]