This review aims to give a comprehensive report of the quinoline ring, related to its therapeutic values. The quinoline and their derivatives have been summarized herein with the IC50 value as per the published research. The importance of the heterocyclic scaffolds has been a hit target of the scientist to synthesize; in view of that bioactive scaffold, the “quinoline” is taken as a reference to give the importance to sensitize the synthesis of the concern bioactive molecule. All quinoline related activity is compiled here as per as our knowledge is a concern. Focuses have been made on significant examples where the impactful activity was reported.