New drug target discovery is currently very popular with a great potential for advancingbiomedical research and chemical genomics. Drug discovery is the process of discovering and designingdrugs that includes target identification, target validation, lead identification, lead optimization andintroduction of the new drugs to the public. G protein-coupled receptors are one of the most important drugtargets. In the current scenario of drug research, approximately 60% of drug target molecules are located atthe cell surface, and half of them are GPCRs. Fragment-based drug discovery is established as analternative approach to high-throughput screening for generating novel small molecule drug candidates.Nanotechnology-based drug delivery systems have seen recent popularity due to their favorable physical,chemical, and biological properties, and great efforts have been made to target nanoDDSs to specificcellular receptors. Protein-protein interactions regulate a wide variety of important cellular pathways, andtherefore represent a highly populated class of targets for drug discovery. An analysis of individual proteinproteininteraction systems has recently yielded success in the discovery of drug-like inhibitors.