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  • Title: The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.
    Author: Tang J, Lackey KE, Dickerson SH.
    Journal: Bioorg Med Chem Lett; 2013 Jan 01; 23(1):66-70. PubMed ID: 23218715.
    Abstract:
    A series of novel, potent 4-aminothienopyridine B-Raf kinase inhibitors was designed and synthesized using knowledge-based design. Compounds 5f, and 6k exhibited not only excellent potency in both enzyme assay (IC(50)=5.1, 16.6 nM) and cellular assay (IC(50)=0.2, 0.2 μM), but also had an outstanding selectivity profile against other kinases.
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