Angewandte Chemie International Edition
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Inside Cover: Seamless Integration of Dose-Response Screening and Flow Chemistry: Efficient Generation of Structure–Activity Relationship Data of β-Secretase (BACE1) Inhibitors (Angew. Chem. Int. Ed. 6/2014)
Structure–activity relationship (SAR) data is a key requirement in modern medicinal chemistry for optimization of lead molecules to drug candidates. In their Communication on page 1704 ff., M. Werner, R. E. Martin, and co-workers demonstrate with beta-secretase that cycle times for SAR generation can be reduced from days to 60 minutes. This accelerated process was achieved by integrating compound synthesis, purification, quantification, and biological assaying into a fully automated flow-based system.