Knowledge Library

Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist

The metabotropic glutamate receptor mGluR7 is widely expressed throughout the CNS and has been implicated in numerous CNS disorders.  WuXi AppTec scientists recently contributed to a study which led to the identification, optimization, and characterization of a highly potent, novel mGluR7 allosteric agonist, designated CVN636.  The authors show that CVN636 has high selectivity toward mGluR7, …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Biochemical Assays, Central Nervous System & Pain, High-throughput screening (HTS), Hit Finding, Hit-to-Lead, Lead Optimization, Small Molecules

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Discovery of Novel GST Inhibitors Identified from a DNA-Encoded Library

WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2. SAR studies, coupled with X-ray crystallography and structural analysis, revealed that …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Biochemical Assays, DNA-Encoded Library (DEL), Hit Finding, Hit-to-Lead, Lead Optimization, Small Molecules, Structural Biology

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One Stop Target-to-Hit Platform: PIK3CA–PIK3R1

Within the PI3K family, the heterodimer protein comprising the p110-α and p85-α catalytic/regulatory subunits (encoded by PIK3CA and PIK3R1) are essential in the regulation of cellular proliferation and carcinogenesis.  To support the discovery of novel PI3K inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and lead optimization …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays, Biophysical Assays, Hit Finding, Hit-to-Lead, Lead Optimization, Oncology, Structural Biology

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One Stop Target-to-Hit Platform: Protein arginine methyltransferase 5 (PRMT5)

Protein arginine methyltransferase 5 (PRMT5) is an enzyme which plays an essential role in a wide range of cellular processes.  PRMT5 overexpression has been implicated in many diseases, including cancer, making this protein an important drug target.  To support the discovery of novel PRMT5 inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays, Biophysical Assays, Hit Finding, Hit-to-Lead, Lead Optimization, Oncology, Structural Biology

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One Stop Target-to-Hit Platform: Cyclin-dependent kinase 2 (CDK2)

Cyclin-dependent kinase 2 (CDK2) and its respective cyclin E1 and cyclin A2 complexes are essential to driving abnormal growth processes in cancer cells, making these proteins important targets for cancer treatment.  To support the discovery of novel CDK2 inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to accelerate hit finding and …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays, Biophysical Assays, Hit Finding, Hit-to-Lead, Lead Optimization, Oncology, Structural Biology

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One Stop Target-to-Hit Platform: Werner Syndrome Helicase (WRN)

Werner syndrome helicase (WRN) is a key drug target for cancers with microsatellite instability.  To support the discovery of potent and selective WRN inhibitors, WuXi AppTec offers a comprehensive platform of biophysical and biochemical assays to support hit finding and lead optimization efforts targeting WRN.  Our panel of services also include high-quality WRN protein production …Read More >

Resource Type: Brochure
Resource Topic: Biochemical Assays, Biophysical Assays, Hit Finding, Hit-to-Lead, Lead Optimization, Oncology, Structural Biology

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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 >

Resource Type: Latest Science, Publication
Resource Topic: Biochemical Assays, Cell-based Assays, Discovery Chemistry, Hit-to-Lead, Lead Optimization, Oncology, Small Molecules

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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 >

Resource Type: Latest Science, Presentation
Resource Topic: Cell-based Assays, Immunology, Lead Optimization

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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

Resource Type: Latest Science, Poster
Resource Topic: Autoimmune and Inflammatory Diseases, in vivo Pharmacology, Lead Optimization, Respiratory Diseases

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Resource Topics
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