In this manuscript, we describe the implementation of a combinatorial apporach to synthesize a library of copper complexes, associated with an activity-based screening to discover the first peptidyl di copper complex mimicking CAT redox chemistry. The selected dinuclear complex was studied in detail and characterized for its CAT activity i<i>n vitro</i> and in cells. Very interestingly, despite moderate intrinsic catalysis constant, this complex was efficacious in a cellular assay.<br>