TUG-770 [Ligand Id: 6483] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2386353 |
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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 | F | 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 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]
