Fragment-based screening is now well-established as a powerful approach to early drug ("lead") discovery.
Diamond is part of several European consortiums, which XChem users can opt into participating.
Once their proposal is approved by Diamond's peer review panel, users should:
iNEXT-Discovery funds access to a wide range of facilities and expert support for translational research in structural biology and life sciences; this supports all European scientists, regardless of prior expertise or familiarity with the methods.
Before coming to DIamond, eligible EU users will be asked to submit an iNEXT proposal (which can be similar to Diamond's proposal) here in order to obtain a PID number.
Brief instruction on how to get a PID number:
European users who do not follow these exact instructions will end up responsible for their own travel and subsistence, which might add up to a substantial cost, due to the nature of the experiment.
The IMI-funded EUbOPEN project offers a route for XChem users to progress fragment hits to high quality potent and specific chemical probes, including automated fragment elaboration chemistry, SAR optimisation, in vitro assay development and cellular validation assays. EUbOPEN members may be able to help with various aspects of progressing fragment hits, depending on the needs of your project. The overall goal of EUbOPEN is to deliver 100 high quality chemical probes that will be freely available to the scientific community and included in online resources such as the chemical probes portal.
Information on how XChem users can collaborate with EUbOPEN and what EUbOPEN may be able to help with is here. To see if your target would fit within the EUbOPEN project or for more information you can contact the EUbOPEN team here.
EU-OPENSCREEN offers another route for XChem users to progress fragment hits. This research infrastructure (RI) integrates high-capacity screening platforms throughout Europe, which jointly use a rationally selected compound collection comprising up to 140.000 commercial and proprietary compounds collected from European chemists. EU-OPENSCREEN offers open access to its shared resources to researchers from academic institutions, SME's and industrial organisations.
The EU-OPENSCREEN fragment library is available to all XChem users; more information on access and conditions are available here.
Possiblities for developing the initial hits into useful chemical matter through EU-OPENSCREEN is detailed here.
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