This review introduces the Structural Chemistry Program at Griffith University's Eskitis Institute, and provides a brief overview over its current and future research portfolio. Capitalising on the co-location with the Queensland Compound Library (QCL), Australia's only small molecule repository, our laboratory investigates the structure and function of proteins with the aim of learning about their molecular mechanisms. Consequently, these studies also feed into drug discovery and design. The thematic focus of our Program is on proteins involved in infection, inflammation and neurological diseases, and this review highlights a few of our recent research efforts in this area.