Fragment-to-Lead Medicinal Chemistry Publications in 2022

Andrew J. Woodhead*, Daniel A. Erlanson, Iwan J.P. de Esch, Rhian S. Holvey, Wolfgang Jahnke, Puja Pathuri

*Corresponding author for this work

Research output: Contribution to JournalReview articleAcademicpeer-review

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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 languageEnglish
Pages (from-to)2287–2304
Number of pages18
JournalJournal of medicinal chemistry
Volume67
Issue number4
Early online date30 Jan 2024
DOIs
Publication statusPublished - 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.

FundersFunder number
Elena Claudia Gini and Louise Walsh
Astex Pharmaceuticals

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