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 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]