Click chemistry is an interesting and novel approach for drug discovery, material science, bioconjugation, radiochemistry and nanoscience. It meets an ever-increasing need for rapid reaction as it fulfills the criterion of an ideal synthesis: efficiency, versatility, selectivity and high yield with variety of starting materials. The present review summarizes all the aspects of 1, 3-dipolar cycloaddition reaction “click reaction” between azides and alkynes catalyzed by copper salts. The ease of purification of products and simplicity of this reaction has opened new pathways in generating vast arrays of compounds with biological potential. Many important reactions fit the concept of click chemistry than others such as cycloaddition of unsaturated species. The present review will outline the deeds of click reaction and its medicinal chemistry application in which click chemistry might be relevant in future.