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Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
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The Current Toolbox for Covalent Inhibitors: From Hit Identification to Drug Discovery.

Mengke You1,2, Hong Liu1,2,3, Chunpu Li1,2,3

  • 1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

JACS Au
|December 26, 2025
PubMed
Summary

New technologies enable targeted covalent inhibitor development for previously undruggable targets. This approach accelerates the discovery of precision covalent therapeutics, enhancing drug selectivity and overcoming resistance.

Keywords:
covalent inhibitordrug designelectrophile screeningtechnology convergenceundruggable targets

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