TUG-905 [Ligand Id: 9149] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2164242
  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
  • 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 8.36 pKi 4.37 nM Ki J. Med. Chem. (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation in presence of 30 uM FFA1 antagonist TUG-761 by dynamic mass redistribution assay F 5.71 pEC50 1949.84 nM EC50 J. Med. Chem. (2012) 55: 6624-6628 [PMID:22724451]
ChEMBL Agonist activity at human GPR40 expressed in HEK293 cells assessed as receptor activation by dynamic mass redistribution assay F 7.34 pEC50 45.71 nM EC50 J. Med. Chem. (2012) 55: 6624-6628 [PMID:22724451]
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 7.85 pEC50 14.13 nM EC50 J. Med. Chem. (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL Agonist activity at human GPR40 expressed in Flp-InTM T-RexTM HEK293 cells assessed as stimulation of calcium mobilization F 8.04 pEC50 9.12 nM EC50 J. Med. Chem. (2012) 55: 6624-6628 [PMID:22724451]
GtoPdb - - 8.05 pEC50 9 nM EC50 J Med Chem (2012) 55: 6624-8 [PMID:22724451]
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 INS-1E cells assessed as receptor activation by dynamic mass redistribution assay F 6.74 pEC50 181.97 nM EC50 J. Med. Chem. (2012) 55: 6624-6628 [PMID:22724451]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL Agonist activity at GPR120 assessed as stimulation of calcium mobilization F 4.36 pEC50 43651.58 nM EC50 J. Med. Chem. (2012) 55: 6624-6628 [PMID:22724451]

ChEMBL data shown on this page come from version 31:

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]