How it works

Fragment-based lead discovery is an innovative drug discovery process that identifies small chemical fragments capable of binding to a target protein. Unlike traditional methods that focus on a few large, complex compounds, this approach explores a broader chemical space relevant to the drug targets of interest. The process involves screening a library of small fragments to find those that bind, even if weakly, to the target protein. Once identified, these fragments serve as starting points for further optimisation and development into more potent lead compounds.

This method increases the likelihood of finding effective drug candidates by providing high-throughput screening of a range of chemical space that is efficient and cost-effective. Additionally, it can be combined with other research techniques to yield even deeper insights.

Typical stages of a Fragment Screening experiment at Diamond

guidelines-diagram

Essential Requirements

If you are providing crystals from your own lab, you will need to have a robust crystallisation system to ensure the success of your fragment screen.  You will need to provide crystals that:

  • Diffract to better than 2.8Å (preferably better than 2.5Å)
  • Are highly reproducible and high yielding – for a full campaign, we will require over 1000 similarly behaved crystals
  • Crystallise in SwissSci_3well plates

Crystallisation Information

In order to reproduce your crystals at Diamond, we need as much information as you can provide about the crystallisation protocol and what we should expect from the crystallisation experiment. We also ask that, in addition to your protein, you ship all solutions required for setting up the crystallisation and any cryoprotectants that will be needed. The following diagram provides an outline of the key information required.  A detailed document will be sent to you prior to conducting your experiment. 

We've created a table outlining the stages of your research, including user requirements, deliverables, and decision points for progressing to the next phase. Click the diagram for more details.

DOWNLOAD >

Want to know more?

Get in Touch