Fragment-Based Hit Screening

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FragmentBuilder - identifying higher quality lead compounds

If you have a pure and well-characterised protein, fragment screening offers a practical and cost-effective alternative to traditional high-throughput screening methods. Our high-throughput fragment-based drug discovery services are designed to provide you with high quality lead compounds at a speed and quality not matched by our competitors.

Exclusive fragment library

Your search needs to be thorough and efficient. That’s why the fragment-based drug discovery team at Domainex have used their significant experience in drug discovery to build their own high quality and unique collection of chemical fragments. The 1,000 fragment library has been designed to provide good coverage of the ‘ideal fragment space’.  The diverse range of pharmacophores make it the ideal starting point for your next drug candidate.

Innovative screening

Domainex is the first contract research organisation in the UK to offer automated MicroScale Thermophoresis (MST) as part of our fragment-based drug discovery services. The high-throughput technique quantifies molecular interactions and structural dynamics, to present binding affinity results in just a few minutes. There are many reasons we think MST offers many advantages over alternative molecular interaction assay methods:

It’s quick

  • Fast, flexible assay set up and a capability of making 400 measurements per hour

It’s sensitive

  • Measurements are carried out in solution, meaning free choice of assay buffer systems and no surface immobilisation of target proteins
  • Broad concentration range (from pM to mM)
  • Live detection of absorption, aggregation and precipitation effects

It’s efficient

  • Small sample consumption (fragment screening using as little as 400µg of protein)

Just the beginning…

We’re confident that our exclusive fragment library and screening techniques will provide you with high quality hit compounds. But that is just the beginning. We can identify soluble domains using our proprietary Combinatorial Domain Hunting platform, and transform hit molecules into clinical candidates using the skills and experience of our medicinal and computational chemists.

If you would like to find out more about fragment based drug discovery including a case study detailing the identification and development of Domainex’s own drug candidate, DMXD-011 (a TBK1/IKKƐ inhibitor), please view our webinar.

View the webinar

If you would like to discuss Domainex’s fragment based drug discovery services, please contact us at enquiries@domainex.co.uk.