High throughput experimentation (HTE) is frequently employed to identify reaction conditions for challenging transformations, giving access to a diverse array of medicinal chemistry targets. In parallel to using conventional batch reactions, we also incorporate flow chemistry into early phase synthesis to help with reaction selectivity and optimization, up-scaling, and solving specific chemical problems. In this …Read More >

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 DEL team, introduces two novel DNA-compatible reactions, successfully incorporating bioactive cores 1,3,4-oxadiazoles and 1,2,4-triazoles into the DEL library. These cores are reported to show broad ranges of biological activities, such as antiviral, anti-inflammatory, anticancer, antifungal, …Read More >

Introduction: Targeted Protein Degradation (TPD) has emerged as a promising therapeutic modality due to its potential to develop therapeutics for previously undruggable targets and address the resistance issues of small molecule inhibitors. Central to this strategy is the novel protein-degradation approach represented by proteolysis-targeting-chimeras (PROTACs), which induce targeted protein degradation through the ubiquitin-proteasome system (UPS). …Read More >

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.  In our latest White Paper, “Emerging Drug Discovery Strategies for Targeted Protein Degradation” we explore how DNA-encoded library (DEL) technology can be used for direct discovery of proteolysis-targeting chimeras …Read More >

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. As of now, over 20 targeted protein degraders have advanced into clinical development. WuXi AppTec has built a robust TPD discovery chemistry platform. We deliver synthetic and medicinal chemistry …Read More >

In this webinar, we present the latest advances and challenges facing researchers focused on new and emerging modalities in drug discovery. Topics include targeted protein degradation, targeted covalent inhibitors, and nucleic acid therapeutics. Our expert speaker, Dr. Tao Guo, discusses solutions for addressing the complexities in designing, synthesizing, and optimizing these molecules, with an added …Read More >

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays. With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition …Read More >

WuXi AppTec scientists collaborated on a study to characterize a series of pyrroloquinoline derivatives that were designed and synthesized to understand the effect of various substitutions on human cytomegalovirus (HCMV) polymerase activity, antiviral activity, and hERG inhibition.  Results suggest that substitutions can be fine-tuned to reduce hERG inhibition while maintaining HCMV antiviral potency. The abstract …Read More >

Learn how parallel medicinal chemistry (PMC) and high throughput experimentation (HTE) combined with machine learning can provide a more focused approach to target molecules, resulting in a more concentrated set of compounds to make the process of lead selection easier. Our experts show how PMC can shorten the turnaround time of the design-synthesis-test cycle, providing …Read More >