CA2668286C — Bruton's tyrosine kinase activity probe and method of using

USPTO Abstract

Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use. The invention relates to a Btk activity probe comprising a Btk inhibitor moiety, a reporter moiety, and a linker moiety that links the inhibitor moiety to the reporter moiety. Specifically described are a Btk inhibitor moiety which covalently bonds to a cysteine residue of a Btk enzyme, a fluorophore and a linker moiety that links the inhibitor moiety to the fluorophore. In an embodiment, the Btk activity probe is: (see compound 3)