TUG-424 [Ligand Id: 3952] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL449588 (4-(2-Toluylethynyl)Dihydrocinnamic Acid)
  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
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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 6.2 pKi 630.96 nM Ki J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
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 7.17 pEC50 67.61 nM EC50 J Med Chem (2016) 59: 4849-4858 [PMID:27074625]
ChEMBL Agonist activity at human FFA1 assessed as calcium mobilization measured for 50 intervals of 0.4 secs by microplate reader analysis F 7.34 pEC50 46 nM EC50 J Med Chem (2013) 56: 982-992 [PMID:23294321]
ChEMBL Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry F 7.34 pEC50 45.71 nM EC50 J Med Chem (2011) 54: 6691-6703 [PMID:21854074]
ChEMBL Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay F 7.34 pEC50 45.71 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]
ChEMBL Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay F 7.49 pEC50 32.36 nM EC50 J Med Chem (2008) 51: 7061-7064 [PMID:18947221]
ChEMBL Agonist activity at human FFA1 expressed in human 1321N1 cells by calcium fluorescence assay F 7.49 pEC50 32 nM EC50 J Med Chem (2008) 51: 7061-7064 [PMID:18947221]
GtoPdb - - 7.5 pEC50 - - - J Med Chem (2008) 51: 7061-4 [PMID:18947221]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay F 5.65 pEC50 2238.72 nM EC50 J Med Chem (2012) 55: 4511-4515 [PMID:22519963]
ChEMBL Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay B 5.84 pEC50 1445.44 nM EC50 ACS Med Chem Lett (2013) 4: 441-445 [PMID:23687558]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]