Small Molecules Archives - Page 2 of 10

Highly Selective Novel Heme Oxygenase-1 Hits Found by DEL

The heme oxygenase (HO) family comprises the major isozymes HO-1 and HO-2, of which HO-1 is deemed as an emerging...

Discovery of Potent, Selective, and Orally Available IRE1 alpha Inhibitors

Inositol-requiring enzyme 1α (IRE1α) is a sensor protein that plays a key role in multiple myeloma (MM) and is a...

Discovery of SARS-CoV-2 Papain-like Protease Inhibitors

SARS-CoV-2 antivirals which have been clinically approved or are in late-stage development are directed against either the RNA-dependent RNA polymerase...

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,...

Recent Advances in HTE and Flow Chemistry

High throughput experimentation (HTE) is frequently employed to identify reaction conditions for challenging transformations, giving access to a diverse array...

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...

Addition of Covalent Warhead and DEL-Generated Hit Fragmentation Empower FBDD

Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds. At the...

DNA-Compatible Cyclizations

The recent publication in the journal Organic Letters, ‘DNA-Compatible Cyclization Reaction to Access 1,3,4-Oxadiazoles & 1,2,4-Triazoles‘ by our WuXi Biology...

STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant...

The contribution of the X-ray crystallography team from our WuXi AppTec site in Germany was acknowledged in a recent study...

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