Medicinal Chemical Biology

Abstract Arguably, the two most important decisions facing drug discovery teams are selecting the target and the therapeutic modality as the focus of their research efforts. This article highlights the recent technical advances in medicinal chemical biology that strongly influence these early, yet centrally important, choices. The article is not meant to be a comprehensive review of all innovations in the area. Examples are chosen that illustrate the impact chemical biology has had recently on drug discovery research. Medicinal chemical biology is ideally suited to expand druggable space through the development of target identification and validation technologies. Equally, innovative therapeutic modalities are required to enhance the medicinal toolkit to ensure that high‐quality clinical candidates are delivered that effectively target pathogenesis. Opportunities and challenges are described that serve to inspire further therapeutic research at the chemistry–biology interface.