L-165461 [Ligand Id: 2690] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL279053 (L-165461) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Agonist activity at PPARalpha | F | 6.24 | pIC50 | 570.16 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | In vitro binding affinity for human PPAR alpha in SPA | B | 6.24 | pIC50 | 570 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Agonist activity at human PPARalpha ligand binding domain expressed in human 293T cells co-transfected with Gal4-DBD by luciferase transactivation assay | B | 5.89 | pEC50 | 1300 | nM | EC50 | J Med Chem (2010) 53: 77-105 [PMID:19928766] |
| ChEMBL | Transcriptional activation by human PPAR alpha | B | 6.61 | pEC50 | 247 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | In vitro binding affinity for human PPAR delta in SPA | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Agonist activity at PPARdelta | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Agonist activity at human PPARdelta ligand binding domain expressed in human 293T cells co-transfected with Gal4-DBD by luciferase transactivation assay | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2010) 53: 77-105 [PMID:19928766] |
| ChEMBL | Transcriptional activation by human PPAR delta | B | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - | J Biol Chem (1999) 274: 6718-25 [PMID:10037770] |
| ChEMBL | In vitro binding affinity for human PPAR gamma in SPA | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Displacement of radio-labeled full agonist from PPARgamma receptor | F | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2011) 46: 2513-2529 [PMID:21482446] |
| ChEMBL | Agonist activity at PPARgamma | F | 6.96 | pIC50 | 109.9 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Agonist activity at human PPARgamma ligand binding domain expressed in human 293T cells co-transfected with Gal4-DBD by luciferase transactivation assay | B | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2010) 53: 77-105 [PMID:19928766] |
| ChEMBL | Transcriptional activation by human PPAR gamma | B | 7.72 | pEC50 | 19 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
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]
