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, RTA402) |
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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 (2017) |
| 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 (2017) |
| 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 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]
