Privileged scaffolds for library design and drug discovery
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This review explores the concept of using privileged scaffolds to identify biologically active compounds through building chemical libraries. We hope to accomplish three main objectives: to provide one of the most comprehensive listings of privileged scaffolds; to reveal through four selected examples the present state of the art in privileged scaffold library synthesis (in hopes of inspiring new and even more creative approaches); and also to offer some thoughts on how new privileged scaffolds might be identified and exploited.
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The fragment binding elements in the authors' initial studies were selected based on their representation in drug-like molecules and were diverse in structure and physicochemical properties.
“The fragment binding elements in our initial studies were selected based on their representation in drug-like molecules14 and were accordingly diverse in structure and physicochemical properties.”
From Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs (2019) · cites this paper as [14]
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- Authors
- Welsch, M. E., Snyder, S. A., & Stockwell, B. R.
- Affiliations
- Columbia University (US)
- Howard Hughes Medical Institute (US)
- Corresponding author
- Snyder, Scott A
- Stockwell, Brent R
- Venue
- Current Opinion in Chemical Biology
- Publisher
- Elsevier BV
- Published
- 2010-06
- Volume
- 14
- Issue
- 3
- Pages
- 347-361
- ISSN
- 1367-5931 (ISSN-L)
- PMC
- PMC2908274
- OpenAlex
- W2162106505
- Cited by
- 1,509
- References
- 49
- Citations by year
- 2026: 83 · 2025: 84 · 2024: 97 · 2023: 101 · 2022: 111 · 2021: 102 · 2020: 109 · 2019: 119 · 2018: 108 · 2017: 114 · 2016: 104 · 2015: 96 · 2014: 91 · 2013: 69 · 2012: 53
- FWCI
- 5.29
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- Locations
- Current Opinion in Chemical Biology (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- Howard Hughes Medical Institute
- Arnold and Mabel Beckman Foundation
- Research Corporation for Science Advancement
- Eli Lilly and Company
- National Cancer Institute (RC2CA148308, R01CA097061)
- National Institute of General Medical Sciences (R01GM084994, R01GM085081, R01-GM84994)
- Topics
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Keywords
- privileged scaffolds, chemical libraries, library design, drug discovery, scaffold-based drug design, chemical library synthesis, bioactive compounds
- MeSH terms
- Pharmaceutical Preparations, Humans, Models, Chemical, Protein Binding, Drug Delivery Systems, Receptors, Cytoplasmic and Nuclear, Small Molecule Libraries, Drug Discovery
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
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