Discovery of an Allosteric, Inactive Conformation-Selective Inhibitor of Full-Length HPK1 Utilizing a Kinase Cascade Assay.
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DOI: 10.1021/acs.biochem.1c00486
Abstract: Achieving selectivity across the human kinome is a major hurdle in kinase inhibitor drug discovery. Assays using active, phosphorylated protein kinases bias hits toward poorly selective inhibitors that bind within the highly conserved adenosine triphosphate… read more here.
Keywords: inhibitor; kinase; discovery; cascade assay ... See more keywords