Bioinorganic chemistry details the function of metal ions in biology or incorporation of metals in pharmaceuticals and imaging agents. Approximately one-third of all enzymes are metalloenzymes, that rely on metal cofactors for structure and function. Studies on metalloenzymes have inspired the synthesis of new catalysts used to achieve many chemical transformations. Metal-containing FDA-approved drugs, including platinum, arsenic, or gold-based drugs have contributed to the improved quality of patient life. Additionally, several imaging agents and radioactive metal compounds remain in active clinical use. In this Methods Collection, the vibrant field of bioinorganic chemistry will be highlighted to provide the scientific community and the broad readership with detailed methods of diverse bioinorganic research. The role of metals in different life processes and disease states as well as the development of metallodrugs and imaging agents will be well described. We will assemble the application of cutting-edge techniques to research at the interface of inorganic chemistry and biology. This Methods Collection has the potential to catapult research advances in this burgeoning field towards significant contributions in medicine.