What are the Advantages of the DEL Technology?
A DNA-encoded library (DEL) of hundreds of millions of molecules can be synthesized by a short combinatorial process and subsequently screened in a single selection experiment against a target protein. This makes it the fastest and most economical approach to hit identification aside from virtual screening. Unsurprisingly, DEL screening has become widely accepted in early drug discovery over the last two decades.
What are the Disadvantages to Overcome?
Despite its acceptance and indisputable advantages, only very few clinical development candidates originate from DEL screening hits. The likelihood of bringing a compound into clinical development correlates with its drug-likeness. Drug-likeness is a measurement based on the physicochemical properties and structural features of a molecule, which are installed during its design and synthesis. The presence of native DNA – as used by everyone in the field – severely limits the type of reactions that can be applied during DEL design and synthesis. As a result, current DELs hardly cover the drug-like chemical space. Converting the subsequent structurally unfavorable screening hits into tractable lead structures amenable to medicinal chemistry is not only laborious, often more than offsetting the original advantage of fast hit identification, but also bears a high risk of failure.
What is SERENGEN's Solution?
SERENGEN utilizes a novel DNA-encoded library technology, which was developed at the TU Dortmund University, Germany. The platform represents a step-change in the synthesis of DNA-encoded libraries. For the first time, a broad range of modern organic synthesis methods can be applied in the presence of DNA. Our unique encoding strategy allows for the synthesis of diverse chemical scaffolds with drug-like structural features and physicochemical properties. Adding drug discovery-proven substituents guarantees that these favorable attributes are kept and the chemical space is sampled in a meaningful manner. Quality control and purification steps during production ensure the delivery of high fidelity DELs, which furnish drug-like hits that can be directly fed into a modern lead generation process. Finally, all advantages inherent to the DEL technology can fully unfold and accelerate hit identification and lead generation.
What are the Unique Advantages of SERENGEN's Technology?
- CeDEC unlocks medicinal chemistry-desired chemical space for DELs.
- The bar coding process is compatible with a wide range modern synthesis methods.
- Application of heterocyclic chemistry becomes compatible with DEL synthesis.
- QC and purification steps ensure high fidelity.
- Designs focus on medicinal chemistry-relevant building blocks.
- Drug-like hits amenable to modern medicinal chemistry accelerating lead generation and optimization.