Journal of the American Chemical Society · 2021 · 95 citations · 47 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryMolecular PharmacologyCovalent Drug DesignCovalent Inhibitor DesignEnzyme InhibitionLigand BindingLigand-based DesignTargeting LigandsBtk InhibitorsCovalent InhibitionCovalent InhibitorsCovalent Kinase InhibitorsFluorescent ProbesTargeted Covalent InhibitorsTargeted Inhibitor DesignThiol Chemistry
. We further demonstrate a BTK CoLDR chemiluminescent probe that enabled a high-throughput screen for BTK inhibitors. Altogether we show that α-substituted methacrylamides represent a new and versatile addition to the toolbox of targeted covalent inhibitor design.
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