seladelpar [Ligand Id: 11137] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL230158 (Mbx-8025, MBX-8025, RWJ-800025, Seladelpar)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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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 Agonist activity at PPARalpha (unknown origin) B 5.82 pEC50 1500 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
GtoPdb Agonist activity determined by cell based transactivation assay. - 6 pEC50 >1000 nM EC50 Bioorg Med Chem Lett (2007) 17: 3855-9 [PMID:17524639]
ChEMBL Activity at human PPARalpha receptor by cell based transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg Med Chem Lett (2007) 17: 3855-3859 [PMID:17524639]
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 (unknown origin) B 8.7 pEC50 2 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
ChEMBL Agonist activity at PPARdelta (unknown origin) B 8.7 pEC50 2 nM EC50 Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
GtoPdb Agonist activity determined by cell based transactivation assay. - 8.72 pEC50 1.9 nM EC50 Bioorg Med Chem Lett (2007) 17: 3855-9 [PMID:17524639]
ChEMBL Agonist activity at human PPARdelta receptor by cell based transactivation assay F 8.72 pEC50 1.9 nM EC50 Bioorg Med Chem Lett (2007) 17: 3855-3859 [PMID:17524639]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Agonist activity at PPARgamma (unknown origin) B 5.3 pEC50 >5000 nM EC50 J Med Chem (2020) 63: 5031-5073 [PMID:31930920]
GtoPdb Agonist activity determined by cell based transactivation assay. - 6 pEC50 >1000 nM EC50 Bioorg Med Chem Lett (2007) 17: 3855-9 [PMID:17524639]
ChEMBL Activity at human PPARgamma receptor by cell based transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg Med Chem Lett (2007) 17: 3855-3859 [PMID:17524639]

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]