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Article

FLiK: a direct-binding assay for the identification and kinetic characterization of stabilizers of inactive kinase conformations.

Methods in enzymology - 1 Jan 2014

Simard Jeffrey R, Rauh Daniel

Abstract excerpt

Despite the hundreds of kinase inhibitors currently in discovery and preclinical phases, the number of FDA-approved kinase inhibitors remains very low by comparison, a discrepancy which reflects the challenges which accompanies kinase inhibitor development. Targeting protein kinases with ATP-competitive inhibitors has been the classical approach to inhibit kinase activity, but the highly conserved nature of the...

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PMID: 25399645
DOI: 10.1016/B978-0-12-397918-6.00006-9

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