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ChEMBL ligand: CHEMBL449588 (4-(2-Toluylethynyl)Dihydrocinnamic Acid) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]