Fragment-based covalent ligand discovery
Open accessAbstract
Covalent fragment-based ligand discovery greatly facilitates the discovery of useful fragments for drug discovery and helps unveil chemical-tractable biological targets in native biological systems.
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Covalent ligand screening from electrophilic compound libraries is becoming more common.
“Covalent ligand screening is another ligand discovery approach that is becoming more common, whereby various methods are used to discover covalent ligands from libraries of electrophilic compounds7,12,13.”
From Advances in covalent drug discovery (2022) · cites this paper as [13]
Over the past decade, covalent ligand discovery has shifted towards screening more drug-like electrophilic fragments.
“Over the past decade, covalent ligand discovery has shifted towards screening more drug-like electrophilic fragments13.”
From Advances in covalent drug discovery (2022) · cites this paper as [13]
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References 121 · Cited by 136
Research works printed but not linked: 7
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- Authors
- Lu, W., Kostic, M., Zhang, T., Che, J., Patricelli, M. P., Jones, L. H., Chouchani, E. T., & Gray, N. S.
- Affiliations
- Harvard University (US)
- Department of Cancer Biology
- Vividion Therapeutics (United States) (US)
- Dana-Farber Cancer Institute (US)
- Corresponding author
- Gray, Nathanael S.
- ORCID
- Venue
- RSC Chemical Biology
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2021
- Volume
- 2
- Issue
- 2
- Pages
- 354-367
- ISSN
- 2633-0679 (ISSN-L)
- PMC
- PMC8341086
- OpenAlex
- W3128963846
- Cited by
- 136
- References
- 121
- Citations by year
- 2026: 27 · 2025: 21 · 2024: 23 · 2023: 34 · 2022: 24 · 2021: 7
- FWCI
- 1.81
- Type
- journal article
- Language
- en
- Update notices
- correction (2021-02-22)
- Open access
- gold
- doi.org
- Licence
- Locations
- RSC Chemical Biology (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Keywords
- targeted covalent inhibitors, chemoproteomics, undruggable proteins, proteome-wide screening
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