Kinases are likely the most well studied target class for discovery, and there are several breakthrough therapies targeting kinases in the oncology space. Two thirds of known kinases are serine-threonine kinases, and about 17% are tyrosine kinases with the remainder classified as atypical kinases. Signaling pathways downstream of various kinases have been well studied, but the challenge for precision drug targeting is the redundancy and overlap of signaling pathways, which can impede therapeutic efficacy. Additionally, loss and gain of function mutations have been identified as disease drivers for several diseases, including various types of cancers.
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At Charles River, we have developed over a hundred assays covering Ser/Thr, Tyr, and lipid kinases utilizing radiometric, fluorescence-based, and luminescent readouts. Our discovery teams have worked on many kinase targets across multiple therapeutic areas, delivering development candidates in inflammation, respiratory, metabolic, and oncology indications. In addition, our pioneering SoftFocus® kinase libraries have been utilized to successfully deliver several development candidates.