Open access chemogenomic library (
https://www.eubopen.org/chemogenomics/chemogenomic-set(odnośnik otworzy się w nowym oknie))
EUbOPEN acquired 2317 candidate compounds covering 975 targets and assessed their purity, structural integrity and cytotoxicity. Specific profiling assays and protocols have been established and published on the EUbOPEN website. New technologies for compound profiling have been developed to speed up the characterization of these compounds.
Chemical probes and ligands (
https://www.eubopen.org/chemical-probes(odnośnik otworzy się w nowym oknie))
In total, 91 chemical tools (chemical probes/handles) from EUbOPEN, EFPIA partners and others partners collaborating with EUbOPEN have been approved by the independent scientific committee and made available to the research community.
The chemical probe effort was supported through recruitment of chemical probes from the research community (academic and private) via the donated chemical probes program. Established partnerships with chemical vendors will maintain the resupply of chemical probes to the research community and ultimately support target identification and development of novel therapeutic strategies.
Chemical probe development was accelerated by parallel protein production, assay development and structural biology efforts as well as by the development of new technologies for hit identification. In four years over 2000 proteins of 628 unique targets have been purified and 25 recombinant antibodies for EUbOPEN target proteins were generated. We established 213 in vitro assays, 139 cellular assays, and 150 CRISPR knockout cell lines to support compound validation. Over 450 protein structures have been deposited in the PDB for public access together with detailed structural descriptions, including material and methods. Further hits have been identified using DNA encoded library screening, fragment screening, Affinity Selection Mass Spectrometry screening, in silico screening, and via contributions from EFPIA partners.
Open access cell assay protocols and data (
https://www.eubopen.org/protocols-reagents(odnośnik otworzy się w nowym oknie))
EUbOPEN has focussed on developing open access cell assay protocols and data from well-characterised human disease tissue to profile the chemical tools in four disease areas: inflammatory bowel disease (IBD), colorectal cancer (CRC), liver fibrosis (LF) and multiple sclerosis (MS), in which patient-derived cell assays (PCAs) for compound screening have been developed and validated. Fifteen tissue assay protocols were established in the four disease areas and made available to the research community together with screening data.
Infrastructure and dissamination of data and materials (
https://gateway.eubopen.org(odnośnik otworzy się w nowym oknie))
In order to facilitate access to the results and outputs of EUbOPEN, we continued to improve and optimise the public-facing Gateway. The Gateway is an interactive tool, which allows searching of data for different user communities, including chemists, biologists and informaticians in a compound or target centric fashion as well as browsing. EUbOPEN compounds have been distributed to laboratories in Europe, North and South America, Australia and Asia. Overall, more than 8,500 compounds have been distributed. Additionally, more than 40 chemical probes are available from commercial vendors.
