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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.

Original publication

DOI

10.1371/journal.pone.0098800

Type

Journal article

Journal

PLoS One

Publication Date

2014

Volume

9

Keywords

Drug Evaluation, Preclinical, Enzyme Activation, Inhibitory Concentration 50, Protein Binding, Protein Kinase Inhibitors, Protein Kinases, Small Molecule Libraries