Protein kinases have proved to be largely resistant to the design of highly specific inhibitors,
even with the aid of combinatorial chemistry. The lack of these reagents has complicated
efforts to assign specific signalling roles to individual kinases. Here we describe a chemical
genetic strategy for sensitizing protein kinases to cell-permeable molecules that do not
inhibit wild-type kinases. From two inhibitor scaffolds, we have identified potent and
selective inhibitors for sensitized kinases from five distinct subfamilies. Tyrosine and …

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