Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This minireview outlines the application of click-chemistry in the synthesis of enzyme inhibitors with the triazole moiety.