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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

  • Kinase Selectivity

    The number of kinases shown to be directly involved in disease processes—either singly or in concert—is growing; as signal transduction pathways continue to be unraveled, more kinases will emerge as potential targets of therapeutic relevance. 

    Therefore, gaining as much information about the kinase profile of an inhibitor is critical and underscores the importance of early-stage profiling against large assay panels. By using a larger kinase panel researchers are afforded a more complete view of compound selectivity, which can assist in uncovering interactions with other therapeutically relevant kinases, thus unlocking greater opportunities for a broader range of clinical applications.  

    Small molecule kinase inhibitors offer considerable promise as therapeutics in a number of chronic and acute diseases.  However, discovery and development of targeted, selective inhibitors remains a challenge.

    KINOMEscan provides a robust high-throughput competitive binding assay platform that allows screening of compounds in parallel as a single experiment using highly standardized assay conditions and reagents. This permits quantitative analysis of compound selectivity and potency against a large number of distinct kinases and important mutant forms as part of a comprehensive kinase inhibitor discovery process.


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