aleglitazar [Ligand Id: 7405] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL519504 (Aleglitazar, R-1439, R1439, Ro-0728804, RO-0728804, RO0728804) |
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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 | Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARalpha expressed in Escherichia coli BL21 cells | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| ChEMBL | Agonist activity at human PPARalpha by luciferase reporter transactivation assay | F | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Agonist activity at mouse PPARalpha | F | 5.63 | pEC50 | 2340 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230] | ||||||||
| ChEMBL | Agonist activity at rat PPARalpha | F | 5.65 | pEC50 | 2260 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Agonist activity at PPARdelta by luciferase reporter transactivation assay | F | 7.28 | pEC50 | 53 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| ChEMBL | Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay | F | 7.68 | pEC50 | 21 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
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]
