Kinases are regulators of a broad range of cellular processes. Deregulated kinase activity is a frequent cause of disease hence kinases are considered attractive targets for drug discovery. As kinase inhibitors mainly share the adenosine triphosphate binding site, an efficient way of finding hits for a new target kinase is by screening a small focussed set of compounds designed to target this pocket. A key issue for translating hits into candidates and medicines for kinases has been that of selectivity over other undesired kinase target activities.This presentation will discuss how a hit compound for PIM1, found through a focussed set screen, and its potential issues of selectivity over GSK3 led to change in kinase profile and a promising selective lead series for PI3Kdelta.

Identification of a selective lead series for a PI3K-delta programme by kinase cross-screening

244th National Meeting (2012)

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