Selectivity assessment of kinase inhibitors: strategies and challenges.
Yan Luo · PubMed · 2005
Most small-molecule kinase inhibitors are ATP competitive, which render them more likely to cross-inhibit other kinases in the same family or even kinases from other families. Assessing compound selectivity is therefore critical for drug development. Recent development of several cutting-edge technologies enabled rapid advances in kinase selectivity assessment and greatly facilitated the industrial drug discovery process.