TUG-905 [Ligand Id: 9149] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2164242 |
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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 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]
