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Nature Reviews Drug Discovery 7, 391–397 (1 May 2008) | doi:10.1038/nrd2541

High-throughput kinase profiling as a platform for drug discovery

David M. Goldstein , Nathanael S. Gray & Patrick P. Zarrinkar

To fully exploit the potential of kinases as drug targets, novel strategies for the efficient discovery of inhibitors are required. In contrast to the traditional, linear process of inhibitor discovery, high-throughput kinase profiling enables a parallel approach by interrogating compounds against hundreds of targets in a single screen. Compound potency and selectivity are determined simultaneously, providing a choice of targets to pursue that is guided by the quality of lead compounds available, rather than by target biology alone.