Related Experiment Video
Updated: Dec 8, 2025

Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
Published on: February 28, 2025
Where Electrophile Signaling and Covalent Ligand-Target Mining Converge
1Swiss Federal Institute of Technology Lausanne (EPFL), CH-1015 Lausanne, Switzerland;,
Abstract:
Interests in learning how to engineer most effective covalent ligands, identify novel functional targets, and define precise mechanism-of-action are rapidly growing in both academia and pharmaceutical industries. We here illuminate the establishment of a multifunctional platform that offers new capabilities to logically engineer covalent ligands and dissect 'on-target' bioactivity with precise biological context and precision hitherto inaccessible. Broadly aimed at non-specialist readers, this opinion piece is aimed to stoke the interest of emerging chemists and biologists/bioengineers, but the underlying technological and conceptual topicality is anticipated to also appeal to experts leading ligand-target mining, validation, and -discovery research programs.
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