The process of drug discovery or lead optimization involves the efficient synthesis of molecules and the creation of chemical libraries. For this reason, the rapid generation of new molecules is essential. Originally defined by Professors Barry K. Sharpless and M. G. Finn in 2001, Click chemistry is a very powerful tool to develop a set of original, selective, and modular building blocks such as azide and alkyne in small and large scales. It is a new type of chemistry that allow to synthesize complex molecules in an efficient way. The applications of this modular approach concern several domains of drug discovery, extending from lead finding through combinatorial chemistry, bionanoparticles, target-template to proteomics and DNA research using bioconjugation reactions. This article summarizes some progress and applications of click chemistry in drug discovery. We also describe the synthesis and characterization of a new triarylmethane prepared in our laboratory using this chemical strategy.