Transformation of in vitro tools for kinase profiling: keeping an eye over the off-target liabilities

Areas Covered: This review provides an overview of traditional biochemical-based kinase profiling as well as an introduction to advances that have been made by moving compound profiling into a cell-based format. Expert opinion: While central to the appropriate prioritization and optimization of compounds during the hit to lead phase of early-stage pharmaceutical development, every compound profiling format must be critically assessed so that one can make informed decisions through an understanding of their strengths and limitations. These decisions will ultimately be balanced against cost, complexity and its biological relevance.