This disclosure reports the development of the first electrochemical-based targeted protein labeling platform within live cells. This technology relies on the use of a minimalist DZE functional group that leverages its intrinsic electrochemical activation properties to generate a reactive intermediate for covalent protein labeling. By appending appropriately functionalized DZE to small molecule ligands of interest, targeted labeling of proteins can be achieved in an electrochemically dependent fashion in both free protein and complex cellular environments. The biocompatibility and reaction