CDDO-Me [Ligand Id: 3443] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1762621 (Bardoxolone methyl, Bardoxolone methyl ester, CDDO-Me, CDDO-METHYL ESTER, NSC 713200, NSC-713200, Rta-402, RTA 402, RTA-402) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Ghrelin O-acyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3588729] [UniProtKB: Q96T53] | ||||||||
| ChEMBL | Inhibition of human GOAT expressed in Sf9 cell membranes assessed as reduction in ghrelin octanoylation pre-incubated for 15 mins before substrate addition and measured after 3 hrs using octanoyl-CoA and fluorescent ghrelin peptide by HPLC analysis | B | 4.64 | pIC50 | 23000 | nM | IC50 | US-20170056373-A1. Ghrelin o-acyltransferase inhibitors (null) |
| Ghrelin O-acyltransferase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255134] [UniProtKB: P0C7A3] | ||||||||
| ChEMBL | Inhibition of mouse GOAT expressed in HEK293FT cells co-expressing pre-proghrelin assessed as reduction in ghrelin octanoylation incubated for 24 hrs by ELISA | B | 7.46 | pIC50 | 35 | nM | IC50 | US-20170056373-A1. Ghrelin o-acyltransferase inhibitors (null) |
| nuclear factor, erythroid 2 like 2/Nuclear factor erythroid 2-related factor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075094] [GtoPdb: 3057] [UniProtKB: Q16236] | ||||||||
| ChEMBL | Activation of Nrf2 (unknown origin) expressed in human HaCaT-ARE-luc cells after 6 hrs by luciferase reporter gene assay | B | 7.22 | pEC50 | 60 | nM | EC50 | J Nat Prod (2017) 80: 2276-2283 [PMID:28753294] |
| signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763] | ||||||||
| ChEMBL | Inhibition of IFN-gamma stimulated STAT3 (unknown origin) expressed in human HeLa cells after 6 hrs by luciferase reporter gene assay | B | 5.62 | pIC50 | 2380 | nM | IC50 | J Nat Prod (2017) 80: 2276-2283 [PMID:28753294] |
| ubiquitin specific peptidase 2/Ubiquitin carboxyl-terminal hydrolase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293227] [GtoPdb: 2430] [UniProtKB: O75604] | ||||||||
| ChEMBL | Inhibition of USP2 (unknown origin) | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2018) 61: 422-443 [PMID:28768102] |
| Ubiquitin carboxyl-terminal hydrolase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157850] [UniProtKB: Q93009] | ||||||||
| ChEMBL | Inhibition of USP7 (unknown origin) using human N-terminal GST-tagged UBA52 as substrate preincubated for 10 mins followed by substrate addition measured after 45 mins by coomassie brilliant blue staining-based SDS-PAGE analysis | B | 4.85 | pIC50 | 14080 | nM | IC50 | J Med Chem (2018) 61: 422-443 [PMID:28768102] |
| Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | 130 | nM | Ki | Mol Endocrinol (2000) 14: 1550-6 [PMID:11043571] |
ChEMBL data shown on this page come from version 33:
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]
