Presentation: 3C02

Protein kinases are attractive targets for drug discovery programs in many disease areas due to the role they play in mammalian signal transduction. At GlaxoSmithKline we have pursued an integrated screening strategy to identify hits and optimize leads, for potency and selectivity, through to candidate selection. In particular, the selectivity profile of inhibitors is key to understanding their effects on signaling networks and understanding cellular effects. A variety of screening technologies are used offering differing advantages. In addition we characterize in detail the mechanism of inhibition of the hits, leads and candidates we identify.

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