Knowledge Library

Fragment-based Drug Discovery

Fragment-based drug discovery is one of the most well-developed approaches for projects starting from small, low-affinity compounds.  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. WuXi AppTec offers a comprehensive fragment screening platform to support hit-to-lead optimization workflows. …Read More >

Resource Type: Brochure
Resource Topic: Fragment-Based Drug Discovery

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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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Pioneering Advanced Modalities in Early Drug Discovery

New modalities such as peptides, oligonucleotides, and cell and gene therapies have revolutionized healthcare industry innovation. To meet these evolving needs, WuXi Biology has proactively developed a broad range of capabilities, offering integrated solutions to global pharmaceutical and biotech companies for challenging targets. We have established major capabilities for new modalities in the early discovery …Read More >

Resource Type: Article
Resource Topic: Antibody Drug Conjugate, CAR-T Cell, Cell Therapies, DNA-Encoded Library (DEL), Fragment-Based Drug Discovery, Gene Therapies, Oligonucleotides, Oncolytic Viruses, Targeted Protein Degradation

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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 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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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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Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

Expansion of the E3 ligase toolbox has the potential to dramatically advance the field of targeted protein degradation.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the discovery of novel small molecule binders of GID4, a substrate receptor in the human CTLH E3 ligase complex.  Researchers used …Read More >

Resource Type: Latest Science, Publication
Resource Topic: DNA-Encoded Library (DEL), Fragment-Based Drug Discovery, Targeted Protein Degradation

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Introduction into Fragment Based Drug Discovery

Fragment-based drug discovery (FBDD) is a method used for finding hit compounds as one strategy of hit identification in the drug discovery process. Fragments are small molecules with a low molecular weight, smaller than lead molecules or druglike molecules. The FBDD technology is based on identifying small chemical fragments, which bind to the biological target …Read More >

Resource Type: Latest Science, Webinar
Resource Topic: Discovery Chemistry, Fragment-Based Drug Discovery, Hit Finding, Hit-to-Lead, Screening Libraries, Small Molecules, Target Identification and Validation

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Resource Topics
× peptide, amino acid

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