Dual binding site inhibitors of B-RAF kinase.

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Wolin RL, Bembenek SD, Wei J, Crawford S, Lundeen K, Brunmark A, Karlsson L, Edwards JP, Blevitt JM

Dual binding site inhibitors of B-RAF kinase.

Bioorg Med Chem Lett. 2008 May 1;18(9):2825-9. doi: 10.1016/j.bmcl.2008.04.002. Epub 2008 Apr 4.

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18434146 [ View in PubMed

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Abstract

Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intended to interact with both the ATP and adjacent allosteric binding domains of B-RAF kinase. Their ability to inhibit the function of B-RAF kinase and intracellular ERK1/2 phosphorylation were evaluated.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sorafenib	RAF proto-oncogene serine/threonine-protein kinase	IC 50 (nM)	3	N/A	N/A	Details
Sorafenib	Serine/threonine-protein kinase B-raf	IC 50 (nM)	15	N/A	N/A	Details