In the field of pharmaceutical science, researchers are constantly seeking for new molecules and construct that exhibit specific properties. While one could easily come up with a structure design that would fit the needs but the real struggle lies in its synthesis and purification. If only readily available structure units could be easily linked together to form numerous molecules of desire in just a few crisp steps. While it still remains a far-reaching dream, click chemistry seems to offer a glimpse of hope. Click chemistry has recently emerged to become one of the most powerful tools in drug discovery, chemical biology and proteomic applications. In recent years, the design and synthesis of pharmacologically relevant heterocyclic molecules by combinatorial techniques have proven to be a promising strategy in the search for new pharmaceutical lead structures. Authors are interested to put current update of click synthesis in the field of enzyme inhibitors and in situ chemistry, in receptor−ligand binding studies, in labeling and Sequencing of DNA, in Site-Specific in Vitro and in Vivo incorporation of molecular probes to study G Protein-Coupled receptors and in design and synthesis of bioorthogonal reagents and nano-particular delivery system. An application of click chemistry in different fields proves effectiveness of click chemistry in lead discovery.
