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 >

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 >

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 >

Mutant p53 is one of the most attractive targets for new anti-cancer drugs. Although traditionally regarded as difficult to drug, several new strategies have recently become available for targeting the mutant protein. One of the most promising of these involves the use of low molecular weight compounds that promote refolding and reactivation of mutant p53 …Read More >

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets, often referred to as targeted covalent inhibitors (TCIs).  In this webinar, experts discuss innovative approaches to screen for covalent binders, strategies for the synthesis of covalent warheads, and assays to optimize the ADME/DMPK properties of these molecules. …Read More >

Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However, because of the continued need for injectable administration, many GLP-1 agonists face compliance challenges. To improve the design and production of GLP-1 receptor biased agonists with enhanced druggability, a novel small molecule, designated SAL0112, was …Read More >

WuXi AppTec scientists contributed to a research article in the journal Nature Microbiology, which characterized a peptidomimetic inhibitor of the SARS-CoV-2 main protease (Mpro).  In a human ACE2 transgenic mouse model, this inhibitor (designated RAY1216) exhibited antiviral activities against SARS-CoV-2 comparable to those of nirmatrelvir, but with improved pharmacokinetics.