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abstractthere is an urgent need for the development of efficient methodologies that accelerate drug discovery . 
 we demonstrate that the strategic combination of fragment linking / optimization and proteintemplated click chemistry is an efficient and powerful method that accelerates the hitidentification process for the aspartic protease endothiapepsin . 
 the best binder , which inhibits endothiapepsin with an ic50 value of 43  m , represents the first example of triazolebased inhibitors of endothiapepsin 
 . our strategy could find application on a whole range of drug targets .