TUG-770 [Ligand Id: 6483] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2386353
  • 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]
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  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
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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 7.07 pKi 85.11 nM Ki J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay in presence of bovine serum albumin B 7.58 pEC50 26.3 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
ChEMBL Agonist activity at C-terminal yellow fluorescent protein-fused human FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay B 7.64 pEC50 22.91 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
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 7.73 pEC50 18.62 nM EC50 J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
GtoPdb - - 8.2 pEC50 - - - ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
ChEMBL Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay F 8.21 pEC50 6.17 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
ChEMBL Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay F 8.22 pEC50 6 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
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 8.23 pEC50 5.89 nM EC50 J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
FFA1 receptor/Free fatty acid receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5411] [GtoPdb: 225] [UniProtKB: Q76JU9]
ChEMBL Agonist activity at mouse FFA1 receptor transfected in human T-REX-293 cells measured for 74 secs by calcium mobilization assay F 6.83 pEC50 147.91 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
FFA1 receptor/Free fatty acid receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795180] [GtoPdb: 225] [UniProtKB: Q8K3T4]
ChEMBL Agonist activity at C-terminal yellow fluorescent protein-fused rat FFA1 receptor transfected in HEK293 cells after 5 mins by BRET assay B 6.49 pEC50 323.59 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay B 6.03 pEC50 933.25 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]

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]