Even though a lot of drug candidates were successful in preclinical stage, most of them would fail to pass clinical trials and get into the market, eventually. At present, phase II success rates are lower than any other phase of development. The main reason why candidates fail in phase II trials is efficacy and safety issues. In most of cases, undesired distribution of the drugs could be considered as one of the main factors to lower efficacy and increase undesired effect. Therefore, efficacious distribution of a potent bioactive molecule without perturbing other tissue could be a solution for increasing phase II success rate, leading to novel drug discovery. The KIM lab has focused on the development of novel drug delivery systems (DDS), based on small molecule-derived organic constructs. In order to successfully achieve the goal, we are trying to use prodrug approaches and small molecule drug conjugates. With theses tools, we are developing innovative DDS for the treatment of chronic inflammatory diseases. We are also interested in the development of diverse theranostic probes which can be used as tools for therapeutics as well as diagnosis.