fasiglifam [Ligand Id: 6484] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1829174 (Fasiglifam, Fasiglifam hemihydrate, Fasiglifam hydrate, TAK-875, TAK875, Tak-875 anhydrous) |
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| 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 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]
