bardoxolone [Ligand Id: 2717] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1093059 (Bardoxolone, CDDO, RTA-401, 2-Cyano-3,12-Dioxooleana-1,9(11)-Dien-28-Oic Acid)
  • Inducible NOS/Nitric oxide synthase, inducible in Human [ChEMBL: CHEMBL4481] [GtoPdb: 1250] [UniProtKB: P35228]
  • Inducible NOS/Nitric oxide synthase, inducible in Mouse [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
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  • Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231]
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  • kelch like ECH-associated protein 1 in Human [GtoPdb: 2757] [UniProtKB: Q14145]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Inducible NOS/Nitric oxide synthase, inducible in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4481] [GtoPdb: 1250] [UniProtKB: P35228]
ChEMBL Inhibition of inducible nitric oxide synthase in activated macrophages B 9.7 pIC50 0.2 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2215-2219 [PMID:15837296]
Inducible NOS/Nitric oxide synthase, inducible in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
ChEMBL Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay B 7.64 pIC50 23 nM IC50 J. Med. Chem. (2015) 58: 4738-4748 [PMID:25965897]
Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231]
GtoPdb - - 8 pKi - - - Mol. Endocrinol. (2000) 14: 1550-6 [PMID:11043571]
kelch like ECH-associated protein 1 in Human [GtoPdb: 2757] [UniProtKB: Q14145]
GtoPdb Measuring inhibition of KEAP1 binding to Cul3 using an AlphaScreen bead-based proximity assay. - 7 pIC50 <100 nM IC50 PLoS ONE (2014) 9: e98896 [PMID:24896564]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]