High-throughput discovery of bioactive small molecules

The discovery of bioactive small molecules (e.g. drugs, agrochemicals, chemical probes) is driven by iterative cycles in which series of molecules are designed, synthesised, purified and tested. The discovery of bioactive small molecules is thus an enduring challenge in both medicinal chemistry and chemical biology. The discovery of biologically-active small molecules tends be both time- and resource-intensive, in part because a similar investment is made in all molecules, irrespective of their ultimate biological activity.

Although automation is widely harnessed within the individual stages of discovery workflows, it is rare for adjacent stages to be integrated, and for all activities to be performed in parallel and with matched throughput. Moreover, a limited reaction toolkit dominates molecular discovery, which has led to an uneven exploration of chemical space and has tended to focus attention on molecules with sub-optimal properties.

This project will establish a high-throughput discovery facility at the Rosalind Franklin Institute, the new national institute dedicated to the development of transformational technologies for the life sciences. The University of Leeds is collaborating with the Rosalind Franklin Institute to achieve a step-change in the efficiency and effectiveness of bioactive small molecule discovery. This will build on many new reactions and chemical approaches that have recently been developed in Leeds to drive the discovery of future drugs and other functional small molecules.


More effective and efficient discovery of new drugs, agrochemicals and chemical probes.

Project website