fasiglifam [Ligand Id: 6484] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1829174 (Fasiglifam, Fasiglifam hemihydrate, Fasiglifam hydrate, TAK-875, TAK875, Tak-875 anhydrous) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 human FFA1 stably expressed in CHO cells assessed as intracellular calcium flux by FLIPR assay | F | 7.21 | pEC50 | 62 | nM | EC50 | Eur J Med Chem (2023) 245: 114883-114883 [PMID:36343410] |
| 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 FFAR1 (unknown origin) | F | 7.28 | pEC50 | 53 | nM | EC50 | Bioorg Med Chem Lett (2021) 41: 127969-127969 [PMID:33771587] |
| 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 expressed in CHO cells measured by FLIPR assay | F | 7.35 | pEC50 | 45 | nM | EC50 | Eur J Med Chem (2022) 229: 114061-114061 [PMID:34954593] |
| 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 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 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 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 GPR40 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay | F | 7.53 | pEC50 | 29.5 | nM | EC50 | Eur J Med Chem (2023) 251: 115267-115267 [PMID:36933395] |
| 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 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 FFA1 (unknown origin) | F | 7.85 | pEC50 | 14 | nM | EC50 | Eur J Med Chem (2023) 245: 114883-114883 [PMID:36343410] |
| 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 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 FFAR1 (unknown origin) | B | 8.11 | pEC50 | 7.7 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1839-1847 [PMID:36518697] |
| 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] |
| FFA1 receptor/GPR40-Galpha16 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL5482994] [GtoPdb: 225] [UniProtKB: O14842, P30679] | ||||||||
| 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 human GPR40/Galpha-16 expressed in HEK293 cells by Fluo4-AM dye based intracellular calcium flux assay | B | 7.45 | pEC50 | 35.8 | nM | EC50 | Eur J Med Chem (2023) 251: 115267-115267 [PMID:36933395] |
| 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 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]
