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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
