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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
  • This target only has 0 pki data point
1 CHEMBL1093059_lig_chart_1 Nitric oxide synthase, inducible HumanMouse
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231]
  • This target only has 1 pki data point
2 CHEMBL1093059_lig_chart_2 Peroxisome proliferator-activated receptor-γ Human
There should be some charts here, you may need to enable JavaScript!
  • kelch like ECH-associated protein 1 in Human [GtoPdb: 2757] [UniProtKB: Q14145]
  • This target only has 0 pki data point
3 CHEMBL1093059_lig_chart_3 kelch like ECH-associated protein 1 Human
There should be some charts here, you may need to enable JavaScript!
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]