A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination

PLoS One. 2014 Jun 10;9(6):e98800. doi: 10.1371/journal.pone.0098800. eCollection 2014.

Abstract

Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening conditions. Furthermore a marked improvement in the correlation was found by using kinase constructs containing the catalytic domain in presence of additional domains or subunits.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Evaluation, Preclinical / methods*
  • Enzyme Activation / drug effects
  • Inhibitory Concentration 50
  • Protein Binding
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinases / chemistry
  • Protein Kinases / metabolism*
  • Small Molecule Libraries

Substances

  • Protein Kinase Inhibitors
  • Small Molecule Libraries
  • Protein Kinases