Features of selective kinase inhibitors.
Article Details
- CitationCopy to clipboard
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