Allosteric inhibitor of USP1, WDR48
Protein target names: USP1, WDR48
Mechanism of action: Allosteric inhibitor
In Vitro Validations
Uniprot ID: O94782
Target Class: Other post-translational modification
Target SubClass: Deubiquitinase
Potency: IC 50
Potency Value: 76 nM
Potency Assay: USP1/UAF1 activity was monitored in a fluorometric ubiquitin−rhodamine110 assay. ML323 also showed IC50s of 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively.
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes, see J. Med. Chem publication for details.
Ubiquitin carboxyl-terminal hydrolase 1, USP1, UBP ...
DOI Reference: 10.1038/nchembio.1455
In Cell Validations
In Vivo Data
No in Vivo Validations
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