Features of selective kinase inhibitors.

Article Details


Knight ZA, Shokat KM

Features of selective kinase inhibitors.

Chem Biol. 2005 Jun;12(6):621-37.

PubMed ID
15975507 [ View in PubMed

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DoramapimodMitogen-activated protein kinase 14Ki (nM)0.097N/AN/ADetails
ImatinibTyrosine-protein kinase ABL1Ki (nM)14N/AN/ADetails
SorafenibSerine/threonine-protein kinase B-rafKi (nM)22N/AN/ADetails
TofacitinibTyrosine-protein kinase JAK3Ki (nM)1N/AN/ADetails