Knowledge Library

TAAR1 as an Emerging Target for the Treatment of Psychiatric Disorders

A growing body of in vitro and in vivo evidence has demonstrated that trace amine-associated receptor 1 (TAAR1) could negatively modulate monoamine transmission and play a crucial role in many psychiatric disorders, including schizophrenia, depression, and anxiety. WuXi AppTec contributed to a review article in the journal Pharmacology & Therapeutics, discussing the current understanding of …Read More >

Resource Type: Latest Science Publication
Resource Topic: Central Nervous System & Pain

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Negative Allosteric Modulation of the µ-Opioid Receptor

DNA-encoded libraries from WuXi AppTec were used in a “steered” screening against either inactive or active μ-opioid receptors in parallel, to find novel negative allosteric modulators of this receptor. The molecule discovered via DEL screening not only shows direct and effective in vitro and in vivo potency, but also helps elucidate the mechanism of negative allosteric modulation of GPCRs. This discovery …Read More >

Resource Type: Latest Science Publication
Resource Topic: Central Nervous System & Pain DNA-Encoded Library (DEL) Hit Finding Small Molecules

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Dianthus Platform: Screening for CRBN-DDB1 Proteolysis-Targeting Chimeras and Molecular Glues

Cereblon (CRBN) forms an E3 ligase complex together with DDB1, CUL4, and RBX1. CRBN functions as a substrate receptor of this complex for the recognition and binding of proteins targeted for ubiquitination and proteasomal degradation.  To support the discovery of CRBN-DDB1 proteolysis-targeting chimeras and molecular glues, WuXi AppTec offers an integrated platform of ready-to-go assays …Read More >

Resource Type: Brochure
Resource Topic: Biophysical Assays Cardiovascular & Metabolic Diseases Central Nervous System & Pain Hit Finding Hit-to-Lead Immunology Infectious Diseases Oncology

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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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Translational Pharmacology of CNS and Metabolic Disorders for Testing New Modality Therapies

Animal studies may provide a close approximation to humans when addressing the key challenge of clinical translatability. In the preclinical setting, new insights into disease models and mechanisms are crucial to efficacy studies. In this webinar, Dr. Deming Xu, Chief Pharmacologist, Executive Director, and Head of In Vivo Pharmacology of WuXi AppTec Discovery Biology will …Read More >

Resource Type: Webinar
Resource Topic: Cardiovascular & Metabolic Diseases Central Nervous System & Pain in vivo Pharmacology Metabolic Diseases NASH Oligonucleotides

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Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors

Dual leucine zipper kinase (DLK) and leucine zipper-bearing kinase (LZK) have emerged as key regulators of neuronal degeneration and axon growth.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry demonstrating the use of ligand- and structure-based drug design approaches to discover an amino-pyrazine chemical series of DLK and …Read More >

Resource Type: Latest Science Publication
Resource Topic: Biochemical Assays Biomarkers Central Nervous System & Pain Discovery Chemistry Lead Optimization Small Molecules

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Ligand Finding and Chemistry Workflows for Targeted Protein Degradation

This webinar will focus on aspects related to PROTAC discovery and chemistry workflows, such as ligand finding strategies, synthesis optimization, and linker design. Successful development of bifunctional molecules requires a deep understanding of multiple processes, including biophysical events which dictate induced proximity and how technologies such as DNA-encoded libraries (DEL) can be leveraged to identify …Read More >

Resource Type: Webinar
Resource Topic: Autoimmune and Inflammatory Diseases Biophysical Assays Cardiovascular & Metabolic Diseases Central Nervous System & Pain Discovery Chemistry DNA-Encoded Library (DEL) Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Structural Biology Target-Specific Assays Targeted Protein Degradation

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Biological Characterization and Development Workflows for Targeted Protein Degradation

This webinar will focus on PROTAC biology workflows, such as in vitro screening assays, in vivo testing, and optimization of DMPK properties. Topics will include the best use of biochemical assays to measure binary/ternary complex formation, cell-based assays to assess target engagement and degradation, strategies for enhancing drug delivery and formulation, and PK/PD evaluation of …Read More >

Resource Type: Webinar
Resource Topic: Autoimmune and Inflammatory Diseases Biochemical Assays Cardiovascular & Metabolic Diseases Cell-based Assays Central Nervous System & Pain Hit-to-Lead in vitro biology in vivo Pharmacology Lead Optimization Oncology Small Molecules Target Identification and Validation Target-Specific Assays Targeted Protein Degradation

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Discovery Newsletter Special New Year Edition 2023

Resource Type: Latest Science Newsletter
Resource Topic: Biophysical Assays Central Nervous System & Pain Discovery Chemistry DNA-Encoded Library (DEL) Hit-to-Lead in silico services Lead Optimization Quantum Mechanics Small Molecules Target Identification and Validation Targeted Protein Degradation

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Resource Topics
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