Electroaffinity Labeling: A New Platform for Chemoproteomic-based Target Identification

07 February 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


Target identification is a critical pillar within the drug discovery process that involves deconvoluting the protein target of a pharmacologically active small molecule ligand. While photoaffinity labeling strategies have become the benchmark for target deconvolution of small molecules owing to their reliance on external activation to induce covalent protein capture, the process of target identification remains one of the most technically challenging aspects of early drug discovery. Thus, there is a strong demand for new technologies that allow for controlled activation of chemical probes to covalently label their protein target. Here, we introduce an electroaffinity labeling (ECAL) platform which leverages the use of a small, redox-active diazetidinone (DZE) functional group to enable chemoproteomic-based target identification of pharmacophores within live cell environments.


electroaffinity labeling
chemical biology
target identification
organic chemistry

Supplementary materials

Supporting information
complete experimental details and all spectra and background data


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