Fragment-to-Lead Medicinal Chemistry Publications in 2022
Andrew Woodhead, Daniel A. Erlanson, Iwan J. P. de Esch, Rhian S. Holvey, Wolfgang Jahnke, Puja Pathuri
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).
Topics & Concepts
ChemistryLead (geology)Fragment (logic)Combinatorial chemistryMedicinal chemistryComputational biologyBiochemical engineeringEngineeringComputer scienceAlgorithmBiologyPaleontologyComputational Drug Discovery MethodsTuberculosis Research and EpidemiologyClick Chemistry and Applications