Strategies for Discovering and Derisking Covalent, Irreversible Enzyme Inhibitors

Johnson, Douglas S, Weerapana, Eranthie, Cravatt, Benjamin F·2010·Future Medicinal Chemistry

Cited by (425)

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  96. BindingDB Entry 50001052: Synthesis and biological activity of peptide proline-boronic acids as proteasome inhibitors.
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  97. BindingDB Entry 50044783: Discovery and structure-activity relationship studies of irreversible benzisothiazolinone-based inhibitors against Staphylococcus aureus sortase A transpeptidase.
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  100. BindingDB Entry 50000297: Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.
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