Abstract
This Perspective is the eighth in an annual series that summarizes successful fragment-to-lead (F2L) case studies published each year. A tabulated summary of relevant articles published in 2022 is provided, and features such as target class, screening methods, and ligand efficiency are discussed both for the 2022 examples and for the combined examples over the years 2015-2022. In addition, trends and new developments in the field are summarized. In 2022, 18 publications described successful fragment-to-lead studies, including the development of three clinical compounds (MTRX1719, MK-8189, and BI-823911).
Original language | English |
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Pages (from-to) | 2287–2304 |
Number of pages | 18 |
Journal | Journal of medicinal chemistry |
Volume | 67 |
Issue number | 4 |
Early online date | 30 Jan 2024 |
DOIs | |
Publication status | Published - 22 Feb 2024 |
Bibliographical note
Publisher Copyright:© 2024 American Chemical Society
Funding
The authors would like to thank Elena Claudia Gini and Louise Walsh from Astex Pharmaceuticals for general discussions and help with cheminformatics analysis.
Funders | Funder number |
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Elena Claudia Gini and Louise Walsh | |
Astex Pharmaceuticals |