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Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
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Exploring Extended Warheads toward Developing Cysteine-Targeted Covalent Kinase Inhibitors

Zheng Zhao1, Philip E Bourne1

  • 1School of Data Science and Department of Biomedical Engineering, University of Virginia, Charlottesville, Virginia 22904, United States.

Journal of Chemical Information and Modeling
|December 10, 2024
PubMed
Summary

Medicinal chemists can now explore new electrophile chemical space for designing covalent kinase inhibitors (CKIs). This study analyzes extended warheads, offering insights to guide CKI development.

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