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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]