Dual binding site inhibitors of B-RAF kinase.
Article Details
- CitationCopy to clipboard
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
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