Features of selective kinase inhibitors

Chem Biol. 2005 Jun;12(6):621-37. doi: 10.1016/j.chembiol.2005.04.011.


Small-molecule inhibitors of protein and lipid kinases have emerged as indispensable tools for studying signal transduction. Despite the widespread use of these reagents, there is little consensus about the biochemical criteria that define their potency and selectivity in cells. We discuss some of the features that determine the cellular activity of kinase inhibitors and propose a framework for interpreting inhibitor selectivity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Drug Evaluation, Preclinical
  • Humans
  • Phosphoric Monoester Hydrolases / metabolism*
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology*
  • Substrate Specificity


  • Protein Kinase Inhibitors
  • Phosphoric Monoester Hydrolases