Knowledge Library

DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2–p53 Inhibitor

Macrocyclic peptides are an emerging molecular class for targeting intracellular protein–protein interactions (PPIs) and for providing an oral modality for drug targets. Herein, we use DNA-encoded cyclic peptide libraries to discover a neutral nonapeptide, UNP-6457, that inhibits MDM2–p53 interaction with an IC50 of 8.9 nM. These studies showcase how tailored DEL libraries can directly yield …Read More >

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

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Biophysical and Structural Biology Methods Enable Fragment-based Covalent Ligand Discovery of Human BTK

Drug Discovery Chemistry Conference 2023 Powerful biophysical and structural biology tools enable the study of large numbers of covalent fragments and are opening up new possibilities in the treatment of various diseases. Here, Dr. Moran Jerabek-Willemsen, Head of Biophysics & Screening in WuXi Biology reports the results of a covalent FBDD project on Bruton’s Tyrosine …Read More >

Resource Type: Presentation Video
Resource Topic: Biochemical Assays Biophysical Assays Discovery Chemistry Fragment-Based Drug Discovery Hit-to-Lead Lead Optimization Mass Spectrometry-based Assays Screening Libraries Small Molecules Structural Biology

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PRMT5-WDR77 Services Platform

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Cells and Protein Science Lead Optimization Structural Biology

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PIK3alpha Services Platform

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Cells and Protein Science Lead Optimization Structural Biology

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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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NLRP3 Services Platform

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Cells and Protein Science Structural Biology

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KRAS Services Platform

Resource Type: Brochure
Resource Topic: Biochemical Assays Biophysical Assays Cells and Protein Science Hit-to-Lead Lead Optimization Structural Biology

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DDC 2023: Biophysical & Functional Characterization of Bifunctional Small Molecules Enables TPD Drug Discovery

Leverage our platform of biophysical methods to accelerate your research on targeted protein degradation. At DDC 2023, WuXi AppTec scientists presented an in-depth panel of assays to support the characterization of bifunctional small molecules. Our cutting-edge services include target protein ubiquitination and degradation assays, techniques to evaluate binary binding, and proximity assays to measure ternary …Read More >

Resource Type: Latest Science Poster
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Hit-to-Lead Lead Optimization Small Molecules Structural Biology Targeted Protein Degradation

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AACR 2023: Integrated platform enables KRAS-targeted drugs discovery

Discover our end-to-end KRAS services platform presented at AACR 2023! WuXi AppTec scientists have established a comprehensive panel of assays on key mutants of KRAS, including G12C and G12D, to empower KRAS-targeted drug discovery. Our suite of services includes 2D/3D cell proliferation assays (utilizing cell lines harboring single or double KRAS mutations) as well as …Read More >

Resource Type: Poster
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Structural Biology Tumor Models

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