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Updated: Jun 3, 2025

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Fragment-to-Lead Medicinal Chemistry Publications in 2023
Rhian S Holvey1, Daniel A Erlanson2, Iwan J P de Esch3
1Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, United Kingdom.
This review highlights successful fragment-to-lead (F2L) studies from 2023, analyzing trends in drug discovery methods and fragment properties. Innovations in NMR, virtual screening, and library design are advancing fragment-based drug discovery (FBDD).
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Biochemistry
Background:
- Fragment-to-lead (F2L) studies are crucial for identifying novel drug candidates.
- Annual reviews track progress and identify emerging trends in this field.
- The 2023 literature provides new insights into F2L methodologies and outcomes.
Purpose of the Study:
- To summarize successful fragment-to-lead (F2L) studies published in 2023.
- To analyze trends in target classes, screening methods, and fragment/lead properties.
- To identify innovations enhancing fragment-based drug discovery (FBDD).
Main Methods:
- Compilation and analysis of 17 F2L studies from 2023.
- Tabulated summary of relevant articles.
- Comparative analysis of 2023 data with historical FBDD trends (2015-2023).
Main Results:
- A comprehensive overview of 16 F2L articles published in 2023.
- Identification of key trends in target classes and screening approaches.
- Analysis of fragment and lead property trends over time.
Conclusions:
- The 2023 literature showcases significant advancements in FBDD.
- Innovations in NMR, virtual screening, fragment library design, and fragment linking are notable.
- These advancements are expected to further improve the success rate of FBDD.
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