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)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Rat [ChEMBL: CHEMBL2129] [GtoPdb: 593] [UniProtKB: P37230]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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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 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]