Stages Archives - Page 2 of 19

Rational Design and Optimization of a Potent IDO1 PROTAC

Indoleamine 2,3-dioxygenase 1 (IDO1) is an enzyme that metabolizes tryptophan, and its activity can lead to immunosuppression, thereby allowing tumors...

Advanced On-bead DEL Technology for Enhanced Drug Discovery Screening

DNA-encoded library (DEL) technology has been recognized as a major screening method with unique advantages for offering vast chemical diversity...

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...

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...

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...

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...

Small Molecule Reactivator of p53 Y220C Mutant

Mutant p53 is one of the most attractive targets for new anti-cancer drugs. Although traditionally regarded as difficult to drug,...

Strategies for Screening and Characterizing Targeted Covalent Inhibitors

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets, often referred...

Pharmacodynamic and Pharmacokinetic Profile of a Novel GLP-1 Receptor Biased Agonist

Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However,...

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