ML364 [Ligand Id: 13057] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3392741
  • ubiquitin specific peptidase 2/Ubiquitin carboxyl-terminal hydrolase 2 in Human [ChEMBL: CHEMBL1293227] [GtoPdb: 2430] [UniProtKB: O75604]
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  • ubiquitin specific peptidase 8/Ubiquitin carboxyl-terminal hydrolase 8 in Human [ChEMBL: CHEMBL2157854] [GtoPdb: 3209] [UniProtKB: P40818]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ubiquitin specific peptidase 2/Ubiquitin carboxyl-terminal hydrolase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293227] [GtoPdb: 2430] [UniProtKB: O75604]
GtoPdb Binding affinity for hUSP2 - 5.28 pKd 5200 nM Kd Sci Transl Med (2023) 15: eadh7668 [PMID:38055802]
ChEMBL Inhibition of human USP2 using Di-Ub IQF as substrate incubated for 15 mins by K63-2 assay B 5.96 pIC50 1100 nM IC50 Eur J Med Chem (2020) 191: 112107-112107 [PMID:32092586]
GtoPdb Inhibition of USP2 de-ubiquitinating activity in vitro - 5.96 pIC50 1100 nM IC50 Sci Transl Med (2023) 15: eadh7668 [PMID:38055802]
ubiquitin specific peptidase 8/Ubiquitin carboxyl-terminal hydrolase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157854] [GtoPdb: 3209] [UniProtKB: P40818]
ChEMBL Inhibition of human USP8 using Di-Ub IQF as substrate incubated for 15 mins by K63-2 assay B 6.02 pIC50 950 nM IC50 Eur J Med Chem (2020) 191: 112107-112107 [PMID:32092586]

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]