Knowledge Library

Screening Methods to Identify RNA-Targeting Small Molecules

RNA molecules are promising drug targets due to their genomic prevalence, disease involvement, and druggable complex structures. Successful examples include RNA-targeting small molecule drugs for spinal muscular atrophy (SMA), with on-going efforts in other RNA-related diseases. Here, Dr. Zhifeng Yu presents our toolbox for discovering RNA-targeting small molecules, with a focus on unique DNA-encoded libraries …Read More >

Resource Type: Webinar
Resource Topic: Biophysical Assays DNA-Encoded Library (DEL) Hit Finding Mass Spectrometry-based Assays

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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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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 >

Resource Type: Article
Resource Topic: DNA-Encoded Library (DEL) Hit Finding Target Identification and Validation

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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 >

Resource Type: Article Latest Science Newsletter
Resource Topic: Cell-based Assays DNA-Encoded Library (DEL) Hit Finding Hit-to-Lead

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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 >

Resource Type: Latest Science Publication
Resource Topic: Cell-based Assays DNA-Encoded Library (DEL) Hit Finding Hit-to-Lead

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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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Discovery of RNA Targeting Small Molecules – Our Toolbox for RNA Drug Discovery

Drug Discovery Chemistry Conference 2023 WuXi AppTec has developed technologies to facilitate RNA small molecule screening, an exciting frontier in drug discovery. SHAPE-MaP is applied to determine RNA structure and dynamics and verify small molecule binding. We utilize the “DNA-Zipper” strategy to enable DNA-encoded libraries to identify RNA binders. With other technologies including fragment-based drug …Read More >

Resource Type: Presentation Video
Resource Topic: Biophysical Assays DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Hit Finding Hit-to-Lead Mass Spectrometry-based Assays Oligonucleotides Small Molecules

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DNA-Encoded Libraries for the Discovery of Small-Molecule Hits

Drug Discovery Chemistry Conference 2023 DNA-Encoded library (DEL) screening is now commonly used in the pharmaceutical industry to find novel chemical matter that modulates protein targets of interest.  Point-by-point, Dr. Alex Satz, Executive Director, WuXi Biology will discuss the primary challenges and limitations of DEL screening, and concisely state the current abilities of the technology …Read More >

Resource Type: Presentation Video
Resource Topic: DNA-Encoded Library (DEL) Hit Finding in silico services Screening Services Small Molecules

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DNA-Encoded Libraries: DELight Handbook

Resource Type: Brochure
Resource Topic: DNA-Encoded Library (DEL) Hit Finding Screening Services Small Molecules

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Resource Topics
× peptide, amino acid

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