Fragment-to-Lead Medicinal Chemistry Publications in 2018

Daniel A. Erlanson*, Iwan J.P. de Esch, Wolfgang Jahnke, Christopher N. Johnson, Paul N. Mortenson

*Corresponding author for this work

Research output: Contribution to JournalArticleAcademicpeer-review

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This Perspective, the fourth in an annual series, summarizes fragment-to-lead (F2L) success stories published during 2018. Topics such as target class, screening methods, physicochemical properties, and ligand efficiency are discussed for the 2018 examples as well as for the combined 111 F2L examples covering 2015-2018. While the overall properties of fragments and leads have remained constant, a number of new trends are noted, for example, broadening of target class coverage and application of FBDD to covalent inhibitors. Moreover, several studies make use of fragment hits that were previously described in the literature, illustrating that fragments are versatile starting points that can be optimized to structurally diverse leads. By focusing on success stories, the hope is that this Perspective will identify and inform best practices in fragment-based drug discovery.

Original languageEnglish
Pages (from-to)4430-4444
Number of pages15
JournalJournal of medicinal chemistry
Issue number9
Early online date8 Jan 2020
Publication statusPublished - 14 May 2020


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