Knowledge Library

Discovery Platform for Targeted Protein Degradation

In the last decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. WuXi AppTec has built a robust TPD discovery platform, allowing for in-depth biological and biophysical characterization of monovalent (molecular glue) and bivalent (PROTAC®) molecules through the use of target …Read More >

Resource Type: Brochure
Resource Topic: DNA-Encoded Library (DEL), Hit Finding, Hit-to-Lead, Mass Spectrometry-based Assays, Targeted Protein Degradation

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In Silico Drug Discovery Platform

WuXi AppTec offers a comprehensive platform of in silico drug discovery services to accelerate the process of hit finding and hit-to-lead optimization.  We provide access to virtual chemical spaces built from our library of novel drug-like scaffolds, to support virtual screening and structure-based virtual screening (SBVS). Advances in ML-empowered virtual screening allows project teams to …Read More >

Resource Type: Brochure
Resource Topic: DNA-Encoded Library (DEL), High-throughput screening (HTS), Hit Finding, Hit-to-Lead, in silico services, Mass Spectrometry-based Assays, Screening Libraries

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Accelerating GPCR Drug Discovery and Development

GPCRs: Function, Structure, and Classifications G protein-coupled receptors (GPCRs) are a prevalent class of transmembrane proteins in animal cells, representing one of the largest families of membrane proteins in mammals. These receptors are widely distributed across numerous organs and regulate physiological functions by stimulating intracellular signaling pathways, thereby influencing cellular behavior. GPCRs have a central …Read More >

Resource Type: Article, Blog
Resource Topic: Biochemical Assays, Cell-based Assays, Hit-to-Lead, in vitro biology

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Integrated Screening in Hit Identification

Despite the availability of modern screening technologies, identification and optimization of hits against poorly druggable targets remains a significant challenge for drug discovery teams.  Generating hit matter and reference compounds with one screening technology and then screening with a second technology has the potential to be a powerful tool for researchers. At this year’s Oxford …Read More >

Resource Type: Latest Science, Poster
Resource Topic: DNA-Encoded Library (DEL), Hit Finding, Hit-to-Lead, Small Molecules

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Addition of Covalent Warhead and DEL-Generated Hit Fragmentation Empower FBDD

Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds.  At the SLAS 2024 meeting in Boston, WuXi AppTec presented a poster reporting on the assembly of a covalent fragment library that is suited to tackle protein targets via serine, lysine, and cysteine residues. In a case …Read More >

Resource Type: Latest Science, Poster
Resource Topic: DNA-Encoded Library (DEL), Fragment-Based Drug Discovery, Hit Finding, Hit-to-Lead, Lead Optimization, Small Molecules

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Covalent Fragment-based Drug Discovery: BTK Inhibitors

At the Covalent Drug Discovery 2023 Summit and Fragments 2024 Conference, we presented a case study on Bruton’s tyrosine kinase (BTK) and demonstrated how biochemical, biophysical, and structural biology methods were used to confirm hits, characterize binding kinetics, and evaluate the mode of interaction of covalent BTK inhibitors. Our hit-to-lead workflow showcases the importance of bioanalytical …Read More >

Resource Type: Latest Science, Poster
Resource Topic: Biochemical Assays, Biophysical Assays, Fragment-Based Drug Discovery, Hit Finding, Hit-to-Lead, Structural Biology

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One Stop Target-to-Hit Platform: CDKs and CDK-Cyclin Complexes

Cyclin-dependent kinases (CDKs) and their cyclin regulatory subunits form complexes that are essential for driving abnormal growth processes in cancer cells, making these molecules important targets for cancer treatment. To support the discovery of novel CDK 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-to-Lead, Lead Optimization, Oncology, Structural Biology

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Biophysical and Structural Biology Methods Enable Fragment-Based Ligand Discovery

Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in the treatment of various diseases. In this webinar, WuXi AppTec presents the results of a conventional and covalent fragment-based drug discovery screen, and our expert speaker discusses how orthogonal biophysical and structural methods enable the …Read More >

Resource Type: Webinar
Resource Topic: Fragment-Based Drug Discovery, Hit Finding, Hit-to-Lead, Lead Optimization

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Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor

DNA-dependent protein kinase (DNA-PK) plays an important role in the overall survival and proliferation of cells, making this enzyme an intriguing target for the treatment of a variety of cancers.  In our latest publication, WuXi AppTec scientists contributed to the discovery and characterization of ZL-2201, a potent and highly selective small molecule DNA-PK inhibitor.  In …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Cell-based Assays, Hit-to-Lead, Lead Optimization, Oncology, Tumor Models

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Resource Topics
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