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Industrial Liaison Group:
Tel: +44 (0) 1235 778797
E-mail: industry@diamond.ac.uk
Fragment screening has become increasingly popular over the last 10 years and is an approach that has revolutionised the drug discovery process.
It provides valuable and cost-effective insights for rational drug design, enabling scientists to identify high-quality lead candidates in the early stages of discovery. Rather than focusing on a few large complex compounds, it explores a larger part of the existing chemical space from the drug targets of interest, providing new entry routes for the development of lead compounds.
At Diamond we provide a fully integrated facility, offering services from crystal cultivation through to targeting, harvesting and data collection & analysis using our high-powered research instruments.
To find out more, visit our Fragment Screening web pages.
Fragment Screening has been playing a major role in the fight against COVID-19. Find out how teams across Diamond have been collaborating internationally to find drug targets to fight the virus.
Read our latest case study outlining the use of Fragment Screening in the fight against COVID-19.
Watch our video to find out how Fragment Screening is changing the face of rational drug design and how it can help in the early stages of the drug pipeline.
Speeding up the drug discovery process has taken a while to achieve, however Fragment Screening promises to do exactly this. In this article Frank von Delft tells us how Diamond's XChem facility delivers a fast, streamlined process with low overheads for its users.
Watch our latest video to find out how Diamond's Fragment Screening platforms can provide an effective and low-cost resource for drug discovery.
On 18th October 2019, our XChem facility on beamline I04-1 diffracted its 100,000th crystal dataset since 2014 - just 1yr for the 2nd 50k! Find out how this technique can advance your research.
In 2017 XChem contributed 35,000 of more than 50,000 crystals imaged on I04-1, but using less than a third of the total beamtime. Find out more about Diamond's amazing integrated facilities, helping to speed up drug discovery through Fragment Screening.
The XChem facility at Diamond provides key information for structure-based drug design. In a recent study we look at how to generate crystals for successful Fragment Screening: Find out more.
Access to the fragment soaking platform and automated data collection at come Diamond has added a further element on top of our diverse internal portfolio of streamlined biochemical, high-content and biophysical screening capabilities at Evotec. Operating through the facility infrastructure and with supporting expertise of Diamond staff we have added significant value to several collaborations this year alone. Most importantly we are delivering information-rich structures to our clients and internal medicinal chemistry teams in a time and cost-effective manner at a critical early phase in the drug discovery pathway.
Dr Paul McEwan, Evotec
Cocktailed fragment screening by X-ray crystallography of the antibacterial target undecaprenyl pyrophosphate synthase from Acinetobacter baumannii DOI: 10.1107/S2053230X19017199
Single-domain antibodies as crystallization chaperones to enable structure-based inhibitor development for RBR E3 ubiquitin ligases DOI: 10.1016/j.chembiol.2019.11.007
Rapid covalent-probe discovery by electrophile-fragment screening DOI: 10.1021/jacs.9b02822
Achieving a good crystal system for crystallographic x-ray fragment screening. DOI: 10.1016/bs.mie.2018.09.027
Gentle, fast and effective crystal soaking by acoustic dispensing DOI: 10.1107/S205979831700331X
The XChemExplorer graphical workflow tool for routine or large-scale protein–ligand structure determination DOI: 10.1107/S205979831700331X
Identifying small molecule binding sites for epigenetic proteins at domain-domain interfaces DOI: 10.1002/cmdc.201800030
Fragment Screening against the EthR-DNA Interaction by Native Mass Spectrometry DOI: 10.1002/anie.201702888
Meet the XChem team, who can support all of your fragment screening needs.
To find out more about Integrated Structural Biology research techniques for Industry, or to discuss potential industrial applications, please make an enquiry, contact the Industrial Liaison team on 01235 778797 or send us an e-mail. You can keep in touch with the latest development by following us on Twitter @DiamondILO or LinkedIn.
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