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From “Intentional Avoidance” to “Resurgence” - Development of Covalent Inhibitors in Drug Discovery

Portrait of Weihao Ma, speaker, with a lab background
Weihao Ma
Graduate Student, Department of Chemistry
University of Georgia
iSTEM Building 2, Room 1218
Organic Seminar

The use of covalent inhibitors in the field of drug discovery has attracted considerable attention in the 2000s. But largely owing to safety concerns, they are rarely considered when initiating a target-directed drug discovery project. Thanks to modern drug discovery approaches, the development of covalent inhibitors has been flourishing in the past decade.

Covalent inhibitors are small molecules with a warhead that form a covalent bond with their targeted enzymes or receptors. A warhead is usually an electrophilic functional group. In this talk, several historical examples of covalent inhibitors and their mechanism of action will be highlighted. Milestones in covalent drug discovery over the past decade will be elaborated and discussion will focus on the basis of discovery approaches taken. Examples for each approach will also be reviewed.


Singh J. J. Med. Chem. 2022, 65, 8, 5886–5901

Nomura, D.K. et al.  Nat Rev Drug Discov 21, 881–898 (2022)

Singh J. et al. Nat Rev Drug Disco 10, 307-317 (2011)

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