SpiroChem AG:
Rosental area, WRO-1047-3
Mattenstrasse 22
4058 Basel, Switzerland
Tel: + 41 61 685 95 00
E-mail: contact@spirochem.com
Swiss Discovery Sciences
DNA-Encoded Libraries technology (DELt) is a recent screening technique used in early discovery for target validation and hit identification. The technology, based on the linkage of a small molecule to an identifier DNA code, allows the screening of billions of compounds simultaneously.
DEL include large collections of small molecules, individually coupled to DNA fragments, serving as amplifiable identification barcodes.
Typically, a core scaffold serves as a centerpiece and has 2 to 4 exit vectors for coupling capping agents (one of them being used to link the DNA fragment).
This means that around each core scaffold, small focused libraries of hundreds of compounds become available and are screened at the same time. The result is a direct read out of an early SAR (Structure-Activity Relationship), which is not possible in a standard HTS. It therefore generates hits that are already very advanced and hopefully require less follow-up chemistry.
Example of preparation of trifunctionalized rigid sp2-sp3 scaffolds by Photoinduced cyclopropanation of indoles with diazo compounds T. C. Fessard, K. Goncharenko, Q. Lefebvre, C. Salomé Chimia 2020, 74, 803-807
At SpiroChem, to expand the limits of the known and bring innovation to the DEL community, we design and prepare novel scaffolds with a particular attention to:
Example of preparation of trifunctionalized rigid sp2-sp3 scaffolds by Photoinduced cyclopropanation of indoles with diazo compounds T. C. Fessard, K. Goncharenko, Q. Lefebvre, C. Salomé Chimia 2020, 74, 803-807
We offer a very diversified set of capping agents with valuable intrinsic properties. They enable fast generation of smart focused libraries of hundreds of compounds which, after testing, will provide valuable early SAR (Structure-Activity Relationship).
Thanks to the design of the core scaffolds and the selection of the capping agents, the generated hits have already advanced properties and hopefully will require less follow-up chemistry and optimization than hits obtained after classical HTS campaigns.