Drug discovery considerations in the development of covalent inhibitors |
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Affiliation: | 1. AbbVie Inc., North Chicago, IL, United States;2. AbbVie Bioresearch Center, Worcester, MA, United States;3. AbbVie Stemcentrx, LLC, South San Francisco, CA, United States |
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Abstract: | In recent years, the number of drug candidates with a covalent mechanism of action progressing through clinical trials or being approved by the FDA has increased significantly. And as interest in covalent inhibitors has increased, the technical challenges for characterizing and optimizing these inhibitors have become evident. A number of new tools have been developed to aid this process, but these have not gained wide-spread use. This review will highlight a number of methods and tools useful for prosecuting covalent inhibitor drug discovery programs. |
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Keywords: | Covalent inhibitor Targeted covalent inhibitor (TCI) Mechanism-based inhibitor Warhead reactivity Activity-based protein profiling (ABPP) Click chemistry |
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