Abstract: The small molecule inhibitors targeting the conserved catalytic function of proteins face such challenges as poor specificity and numerous side-effects, while targeting the non-catalytic functions of proteins has great potential for the development of drugs. In view of the wide prospects of inhibitors targeting the non-catalytic functions of proteins, this review briefly summarizes the new drug discovery strategies in this field, including non-catalytic functional domain strategy and the strategies of allosteric regulation and protein-protein interaction, with a prospect of their existing problems and future application, aiming to provide new directions for the development of drugs targeting the non-catalytic functions of proteins.