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Updated: Nov 20, 2025

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
Published on: February 28, 2025
Covalent inhibitors: a rational approach to drug discovery
Fandi Sutanto1, Markella Konstantinidou1, Alexander Dömling1
1Department of Pharmacy , Group of Drug Design , University of Groningen , A. Deusinglaan 1 , 9713 AV , Groningen , The Netherlands . Email: a.s.s.domling@rug.nl ; http://www.drugdesign.nl.
Abstract:
Covalent inhibitors are recognized as an important component in drug discovery and therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the field has advanced significantly and currently about 30% of the marketed drugs are covalent inhibitors. The numerous advantages of covalent inhibitors are counteracting the initial concerns regarding potential off-target toxicity. Thus, continuous research, especially for cancer targets is reported. The aim of this review is to provide a short historic overview and focus on recently developed covalent inhibitors (2011-2019), including structural aspects and examples on challenging targets.
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