compound B [PMID:18477808] [Ligand Id: 3367] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL604126 |
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| 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 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 | 7.16 | pKi | 69.18 | nM | Ki | J Med Chem (2016) 59: 4849-4858 [PMID:27074625] |
| GtoPdb | - | - | 6.1 | pEC50 | - | - | - | Diabetes (2008) 57: 2211-9 [PMID:18477808] |
| ChEMBL | Agonist activity at human FFA1 transfected in 1321N1 cells assessed as calcium mobilization by microplate assay | F | 6.75 | pEC50 | 177.83 | nM | EC50 | ACS Med Chem Lett (2010) 1: 345-349 [PMID:24900217] |
| ChEMBL | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry | F | 7.06 | pEC50 | 87.1 | nM | EC50 | J Med Chem (2011) 54: 6691-6703 [PMID:21854074] |
| 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 | 7.26 | pEC50 | 54.95 | nM | EC50 | J Med Chem (2016) 59: 4849-4858 [PMID:27074625] |
| ChEMBL | Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSA | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1298-1301 [PMID:20064714] |
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]
