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Mar 1, 2009 (Vol. 29, No. 5)

TechNote: High-Throughput Kinase Selectivity Profiling

Bridging the Gulf between Compound Libraries and Rapid Discovery

  • Protein kinase-focused drug discovery efforts are escalating rapidly as research continues to elucidate and define the role of kinases in a growing list of diseases. To date, these research efforts have yielded eight FDA-approved small molecule kinase inhibitors with over 500 more in active development. While kinase inhibitors demonstrate great promise for disease treatment and management, target selectivity is a common challenge in drug development. 

    High-throughput screening in kinase inhibitor discovery is an effective platform for hit identification, compound annotation, and selectivity profiling. In the traditional kinase inhibitor discovery paradigm, however, a compound library is typically interrogated against a single kinase.

    The disadvantage with this approach is that it may overlook off-target interactions that may be important for understanding biological activity. Additionally, only a limited view of a library’s kinome-wide inhibition potential is provided, which may prevent identification of other therapeutically relevant interactions. 

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