A comprehensive approach to X-ray crystallography for drug discovery at a synchrotron facility — The example of Diamond Light Source

•Drug discovery relies on quick and reliable MX experiments.•Innovation at Diamond has increased throughput and quality of crystallographic data.•Diversification of beamline offer expands the landscape of drug targets that can be studied.•Integrated facilities and non-MX instruments give a comprehensive structural investigation.•Industrial partners have been pivotal to the development of MX at Diamond. A detailed understanding of the interactions between drugs and their targets is crucial to develop the best possible therapeutic agents. Structure-based drug design relies on the availability of high-resolution structures obtained primarily through X-ray crystallography. Collecting and analysing quickly a large quantity of structural data is crucial to accelerate drug discovery pipelines. Researchers from academia and industry can access the highly automated macromolecular crystallography (MX) beamlines of Diamond Light Source, the UK national synchrotron, to rapidly collect diffraction data from large numbers of crystals. With seven beamlines dedicated to MX, Diamond offers bespoke solutions for a wide variety of user requirements. Working in synergy with state-of-the-art laboratories and other life science instruments to provide an integrated offering, the MX beamlines provide innovative and multidisciplinary approaches to the determination of structures of new pharmacological targets as well as the efficient study of protein-ligand complexes.