Knowledge Library
On-bead DEL Application and Case Study for Drug Discovery
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 >
Discovery of a Novel Covalent Inhibitor Using DEL
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 >
DEL Screening to Discover Small Molecule Ligands for RNA
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 >
Discovery of a Selective BET Inhibitor for Treating Osteoarthritis
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 >
Discovery of GuaB Inhibitors for the Treatment of Tuberculosis
Tuberculosis is the leading cause of death from an infectious disease and is caused by Mycobacterium tuberculosis (MTB). Inosine-5′-monophosphate dehydrogenase (GuaB) is an enzyme that performs the rate-limiting step in the de novo biosynthesis of guanine, which is critical for growth of bacteria, including MTB. The development of a novel antibiotic that inhibits GuaB could …Read More >
Discovery Platform for Targeted Protein Degradation
In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. WuXi AppTec has built a robust TPD discovery platform, allowing for in-depth biological and biophysical characterization of monovalent (molecular glue) and bivalent (PROTAC®) molecules through the use of target …Read More >
In Silico Drug Discovery Platform
WuXi AppTec offers a comprehensive platform of in silico drug discovery services to accelerate the process of hit finding and hit-to-lead optimization. We provide access to virtual chemical spaces built from our library of novel drug-like scaffolds, to support virtual screening and structure-based virtual screening (SBVS). Advances in ML-empowered virtual screening allows project teams to …Read More >
Creating a Biological Switch Using DEL Technology
In addition to identifying chemical starting points for early drug discovery processes, DNA-encoded library (DEL) technology has now expanded to new applications, including the discovery of bifunctional affinity ligands historically considered difficult to develop. At the 2024 Gordon Research Conference, WuXi AppTec presented a poster describing how DEL can enable the rapid discovery of novel …Read More >
Integrated Screening in Hit Identification
Despite the availability of modern screening technologies, identification and optimization of hits against poorly druggable targets remains a significant challenge for drug discovery teams. Generating hit matter and reference compounds with one screening technology and then screening with a second technology has the potential to be a powerful tool for researchers. At this year’s Oxford …Read More >