Features of selective kinase inhibitors.

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Knight ZA, Shokat KM

Features of selective kinase inhibitors.

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

PubMed ID

15975507 [ View in PubMed

]

Abstract

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

Drug	Target	Property	Measurement	pH	Temperature (°C)
Doramapimod	Mitogen-activated protein kinase 14	Ki (nM)	0.097	N/A	N/A	Details
Imatinib	Tyrosine-protein kinase ABL1	Ki (nM)	14	N/A	N/A	Details
Sorafenib	Serine/threonine-protein kinase B-raf	Ki (nM)	22	N/A	N/A	Details
Tofacitinib	Tyrosine-protein kinase JAK3	Ki (nM)	1	N/A	N/A	Details