The XXIst International Symposium on Medicinal Chemistry from the European Federation of Medicinal Chemistry (EFMC-ISMC), held in Brussels, included topics covering new therapeutic developments in the field of medicinal research. This conference report highlights selected presentations on therapies for neuropathic pain, cognitive disorders, cancer and infection. Investigational drugs discussed include the anticancer imidazole derivative IRC-083927 (Ipsen), the HCV protease inhibitor TMC-435 (Tibotec Pharmaceuticals) and the tuberculosis therapy bedaquiline (Tibotec Pharmaceuticals).