The kits improve signal-to-noise ratios and reduce false positives as well as providing rapid access to broad chemical space for identification of medicinal chemistry starting points
Merck and DyNAbind GmbH have signed an exclusive agreement for the global distribution of fragment-based DNA-Encoded Library (DEL) kits to accelerate drug discovery applications.
In partnering with DyNAbind GmbH to bring an off-the-shelf DEL library to the market, Merck continues to accelerate drug discovery globally. Through our products and services, customers are increasingly able to navigate the early discovery workflow; traditional strengths in medicinal chemistry reagents are complemented by retrosynthetic software, chemical biology tools and now, ready-access to DEL technology for Hit and Lead Discovery.
The DEL kit, containing more than 370,000 paired arrangements of molecular fragments, provides drastically improved signal-to-noise ratios and reduced false positive hit rates, precluding lengthy hit validation steps and allowing for meaningful results in days instead of months. The kit also includes customer access to a secure analysis portal. Hosted by Merck, this portal enables deconvolution of the DNA sequence to reveal the chemical identity of the fragment or fragment-pair hits.
Unlike traditional high-throughput screening methods which require sophisticated robotics equipment and specialised biochemical assays, DELs offer a low-footprint solution that can be used in any laboratory with regular molecular biology equipment.
DyNAbind’s Dynamic Libraries are built on a novel DNA architecture that allows the formation of randomised, transient pairs of chemical structures. These pairs reshuffle in solution until stabilised by binding to the target protein, offering in situ generation of additional copies of the most strongly binding pairs for better signal-to-noise ratio and reduced false positive hits.
The chemical structures available in the kit were carefully selected to ensure maximum diversity and medicinal chemistry relevance. Before being integrated into the library, each molecule was cross-checked to prevent the inclusion of toxic or promiscuously binding substructures, while strict cutoffs were applied to physicochemical properties.
The fragment-based technology provides both an easy access point to DEL technology for new users and value to groups already engaged in traditional DEL technology by accessing a different structural type of potential hits. Additional kits will follow.