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Updated: Oct 25, 2025

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
Published on: February 28, 2025
Recent advances in the development of covalent inhibitors
Hyunsoo Kim1, Yoon Soo Hwang1, Mingi Kim1
1CRI Center for Chemical Proteomics, Department of Chemistry, Seoul National University Seoul 08826 Korea sbpark@snu.ac.kr.
Abstract:
The use of covalent inhibitors in the field of drug discovery has attracted considerable attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market, and numerous covalent drug candidates are now under development. Therefore, interest in covalent drugs is expected to continue in the future. The purpose of this focused review is to provide an understanding of the development of covalent inhibitors by describing their inherent characteristics, possibilities, and limitations based on their mechanistic differences from noncovalent inhibitors. We also introduce the latest covalent warheads that can be applied to the development of potential covalent inhibitors.
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