Hit validation is a crucial step in drug discovery based on DNA-encoded libraries (DEL). Rapid and accurate resynthesis of compounds, along with subsequent validation, can significantly accelerate the drug discovery process. The groups of Professors Jörg Scheuermann and Renato Zenobi from ETH Zurich developed a new method for validating on-DNA compounds with the support of …Read More >

The ATP-adenosine pathway plays a crucial role in regulating immune responses, including those involved in combating tumors. CD39 is an enzyme that breaks down ATP into adenosine. Adenosine, in turn, can suppress the immune system, potentially hindering the body’s ability to fight cancer. By inhibiting CD39, researchers aim to increase ATP levels in the tumor …Read More >

In our latest publication, WuXi AppTec scientists introduce two new methods that utilize readily accessible aldehydes to create substituted isoxazolines and isoxazoles by the 1,3-dipolar cycloaddition reaction. Isoxazoles and isoxazolines, known for their diverse bioactivities—including antibacterial, antifungal, and insecticidal properties—are now accessible through a novel DNA-compatible method developed in this study. This approach enables the …Read More >

DNA-encoded library (DEL) technology has been recognized as a major screening method with unique advantages for offering vast chemical diversity and multiplexed affinity-based screening. Recently, solid-phase On-bead DEL, also known as one bead one compound (OBOC), has been developed to further expand DEL screening from affinity-based screening into biochemical activity screening. At the 2025 SLAS …Read More >

Chemical inducers of proximity (CIPs) are small molecules that induce the proximity of two biological targets, usually proteins. Molecular glues and PROteolysis TArgeting Chimeras (PROTACs®) are among the best-known CIPs. These molecules utilize the endogenous E3-based proteolysis pathway to induce proximity between the target protein and E3 ligase, thereby triggering targeted protein degradation. At the …Read More >

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets. Covalent drugs have the potential to provide enhanced potency and prolonged duration of action compared to non-covalent drugs. Emerging areas of interest include the development of reversible covalent inhibitors, covalent degraders, and covalent targeting of non-cysteine amino …Read More >

RNA-targeted therapeutics are highly intriguing due to their unique physiological properties and novel modes of action in drug R&D. Developing methods to target RNA can lead to new therapeutic options, especially for conditions where RNA plays a pivotal role, such as genetic disorders, viral infections, and cancer. Over the past decade, discovering novel chemical matter …Read More >

Bromodomain and extra-terminal domain (BET) family proteins are key regulators of gene transcription and have been implicated in a wide range of diseases, making these proteins a potential therapeutic target.  Abnormal BET protein activity has been linked to cancer, inflammatory disorders, viral infections, and neurodegenerative conditions. In a recent publication, researchers highlight the discovery of …Read More >

Currently, there is a lack of efficient experimental strategies to collect high-quality proteome level data for protein-ligand interactions (PLIs).  At the 2024 ML Drug Discovery Symposium, WuXi AppTec presented a poster showcasing our advanced DELvision database, representing the first use of DNA-encoded library (DEL) technology for establishing a protein-DEL interaction database. The authors demonstrate how …Read More >