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Abstract
Background: The increasing number of kinases as potential drug targets, in combination with the need to screen large compound collections, demands the kinase assays to be homogeneous, non-radioactive, robust, sensitive, easy to miniaturize, and high-throughput. Objective: This review will focus on some of the chief biochemical and cellular kinase assay technologies and their applications in tyrosine kinase drug discovery. Methods: Recent literatures on these tyrosine kinase assay technologies are reviewed, each assay principle, advantages and drawbacks, as well as their potential utilities in tyrosine kinase drug discovery are discussed. Results/conclusion: There is no perfect assay yet; the choice of assay technology relies on the consideration of many factors including the intrinsic properties of the assay, intended application, cost, timeline, synergy with other in-house assay technologies and the expertise, familiarity and comfort level with certain technologies.