Knowledge Library
DELvision: Improving Data-Driven Drug Discovery
DELvision is a powerful DNA encoded library (DEL)-based toolset for AIphaFold-assisted drug discovery and target sciences. In contrast to conventional screens where the target space is low-dimensional, DELvision comprises a high-dimensional map of binding relationships between small molecules and protein targets. As such, this rich data universe enables simultaneous characterization of targets and exploration of …Read More >
New study by Promega and WuXi AppTec demonstrates novel chemical probes from DELs
As reported in Business Wire: DNA-Encoded Libraries (DELs) and NanoBRET Target Engagement Assays Accelerate Drug Discovery: “The authors demonstrate that DELs can benefit chemical biologists who require verification of live cell target engagement for their protein of interest. This is particularly beneficial for understudied protein classes that may not have existing chemical probes. Additionally, they …Read More >
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)
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 >
DELs enable the development of BRET probes for target engagement studies in cells
WuXi AppTec scientists recently contributed to a research article in Cell Chemical Biology demonstrating the successful conversion of ligands identified from DNA-encoded library (DEL) screening into highly functional, cell-active, bioluminescence resonance energy transfer (BRET) probes. The authors show that analyzing preliminary DEL hits based on target occupancy data generated in live, intact cells is an …Read More >
In Vitro Immunology Assay Platform
Leverage our panel of in vitro immunology assays to accelerate your lead optimization efforts. WuXi AppTec offers a comprehensive platform of immune profiling services, including ligand/receptor binding for target validation and cell-based functional assays to characterize both innate and adaptive immune responses. Our end-to-end services panel includes suppressive assays, mixed lymphocyte reactions, mast cell degranulation assays, …Read More >
CD34+ Hematopoietic Stem Cell Differentiation Platform
To accelerate screening and lead optimization efforts involving immune cell differentiation, WuXi AppTec offers a comprehensive CD34+ hematopoietic stem cell differentiation platform. Our panel includes neutrophil, eosinophil, erythroid, and mast cell differentiation, as well as monocyte/macrophage differentiation and polarization, and megakaryocyte/platelet differentiation. Check out our comprehensive platform of immune profiling and biomarker services
Inhibition of the hERG potassium ion channel by non-nucleoside CMV polymerase antiviral inhibitors
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 >
AACR 2023: Comparison of two DTH models for T cell-mediated immunity
To characterize the immunity profile of the most widely used delayed-type hypersensitivity (DTH) models, WuXi AppTec scientists built 2,4-dinitrofluorobenzene (DNFB) and oxazolone-induced DTH models in both BALB/c and C57BL/6 mice with robust ear thickness as the readout. Check out our comprehensive panel of services related to autoimmune and inflammatory diseases
Recent Advances in Library Synthesis to Accelerate Medicinal Chemistry Research
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 >