Dual binding site inhibitors of B-RAF kinase.

Article Details

Citation

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.

PubMed ID
18434146 [ View in PubMed
]
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
DrugTargetPropertyMeasurementpHTemperature (°C)
SorafenibRAF proto-oncogene serine/threonine-protein kinaseIC 50 (nM)3N/AN/ADetails
SorafenibSerine/threonine-protein kinase B-rafIC 50 (nM)15N/AN/ADetails