SOLUTIONS & SERVICES Screening Technologies Screening Technologies Since Edelris’ inception, we have pioneered the design and production of unique and bio-relevant Keymical Collections™, relying upon chemical tractability, optimized physchem properties and strong IP-potential. Many hit-to-lead success stories of our customers originate from structures found in these collections. Thrilled by this unmatched potential and building upon our long-standing expertise, we have pushed the limits up to a truly increased chemical space coverage, assembling a multi-million compounds proprietary Keymical Space™, for both wet or virtual screening applications. Affinity Selection – Mass Spectrometry (AS-MS) It is possible for our clients to combine this chemical space with our Affinity Selection – Mass Spectrometry (AS-MS) screening platform. Unique results have been obtained from this discovery engine on difficult-to-drug targets, setting up new standards for our clients’ quest to innovative ligands. If you have difficult-to-drug targets, and are willing to beneficiate from EDEN (Edelris Discovery ENgine), do not hesitate to reach out to us! The main advantages of the Edelris AS-MS screening platform are: Straightforward screening setup: Fast track assay development, since AS-MS methods are solution based and do not require immobilization steps. Limited false positives, accelerating direct ligand identification via high resolution mass detection and optimized screens. Our screening deck is assembled without any chemistry limitations, as the compounds do not need any additional and labile tags. Mass-encoded compounds designed and synthesized by EDELRIS, using current medicinal chemistry guidelines. Unique and diverse compound deck (2 Millions) originating from EDELRIS’ own manufactured sp3-rich and diverse Keymical SpaceTM. Very quick re-synthesis of active hits for confirmation as singles using in-house building blocks and team of expert chemists. High flexibility in decks to be screened: You can also opt for the screening of your own corporate decks. The entire process is performed in Edelris laboratories, from target qualification to deliverables sent to clients. This provides high confidence of ligand identification and delivery within 4 months. In addition, competition assays can be easily carried out using the AS-MS technology and allow to determine whether hits are in exclusive binding with reference compounds. It also enables to classify hits in groups according to their binding sites and mode. Kd can also be determined allowing for hit ranking according to their target affinity. Applicable targets include GPCRs, Kinases, G-proteins, Transcription factors, Hydrolases, Membrane proteins, PCSK9, Sting, ncRNA riboswitch, cytoskeleton enzymes,… For more information on the AS-MS technique consult our « Nature Review Chemistry » perspective from 2020 co-authored by Renaud Prudent, Didier Roche and Jean-Yves Ortholand (Edelris) with Allen Annis (Aileron Therapeutics) and Peter Dandliker (Dewpoint Therapeutics). Keymical Space™ & Virtual Screening Structural information has reached a prominent role in drug discovery as a key experimental design tool. The EDEN platform (Edelris Discovery ENgine) relies on Edelris’ proprietary Keymical Space™ (>10 M original structures) and virtually screens innovative molecular frameworks on challenging targets. Based upon Edelris’ medicinal chemistry know-how of NP and NP-like sp3-rich molecules, the virtual hits identified can be rapidly converted into discrete compound libraries for biological evaluation. This approach has been validated with success on several R&D projects conducted on behalf of clients. One of the most desirable tasks following identification of virtual hits after a virtual screening (VHTS) campaign is to transform them as quickly as possible into real samples accessible off the shelf or via chemical synthesis, and to test them in the relevant bio-assay for confirmation. Legal notice Credits Phone: +33 (0)437 561 900 60, Avenue Rockefeller, Bioparc, Bioserra 1 Building, 69008 LYON, FRANCE