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]
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 32:

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]