Fragment-based Drug Discovery

The secret of success in drug discovery written by the pioneers in the field with unrivaled experience in fragment-based methods.In this handbook, the first-hand knowledge imparted by the world's leading experts provides a comprehensive overview of current methods and applications of fragment-based discovery. The first part discusses basic considerations concerning when to use such methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel, and emerging techniques for fragment screening, including empirical as well as computational approaches, while also discussing such special cases as complex target systems and covalent inhibitors. The third and final part presents a number of successful real-world studies from recent and on-going drug discovery projects relating to a variety of target classes, from kinases and phosphatases to beta-secretase and epigenetic targets.With its discussion of future developments and potential novel applications, this will remain a valuable reference source for years to come.