Thank you for visiting nature.com. You are using a browser version with limited support for CSS. To obtain
the best experience, we recommend you use a more up to date browser (or turn off compatibility mode in
Internet Explorer). In the meantime, to ensure continued support, we are displaying the site without styles
and JavaScript.
Advances in areas such as microfluidics-assisted chemical synthesis and biological testing, as well as in artificial intelligence systems, are increasingly providing opportunities to introduce greater automation into the small-molecule drug discovery process. Schneider highlights approaches and technologies that seem poised to be implemented robustly by medicinal chemists in the near future and analyses the challenges for their more widespread application
Recent advances in areas such as natural product biosynthesis, synthetic biology and the development of biosensors are providing new opportunities to directly harness evolutionary pressure to identify and optimize compounds with desired bioactivities. This article describes innovations in the key components of such strategies, highlights pioneering examples that indicate their potential, and discusses the scientific gaps and challenges that remain to be addressed to realize this potential more broadly in drug discovery.