Fragment-to-Lead Medicinal Chemistry Publications in 2023
Rhian S. Holvey, Daniel A. Erlanson, Iwan J. P. de Esch, Barbara Farkaš, Wolfgang Jahnke, Tsuyoshi Nishiyama, Andrew Woodhead · Journal of Medicinal Chemistry · 2025
This Perspective summarizes successful fragment-to-lead (F2L) studies that were published in 2023 and is the ninth installment in an annual series. A tabulated summary of the relevant articles published in 2023 is provided (17 entries from 16 articles), and a comparison of the target classes, screening methods, and overall fragment or lead property trends for 2023 examples and for the combined entries over the years 2015-2023 is discussed. In addition, we identify several trends and innovations in the 2023 literature that promise to further increase the success of fragment-based drug discovery (FBDD), particularly in the areas of NMR and virtual screening, fragment library design, and fragment linking.