Modern Approaches in Drug Discovery, Volume 611, the latest release in the Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting chapters on topics such as Target Identification and Validation, Cell Painting/High Content Imaging, Target ID using chemical probes, Mining the microbiome for targets, Data driven approaches for diversity and drug-likeness, Affinity-based screening, Fragment screening (X-ray), Array-based approaches, Hit-to-lead: assessment and improvement of drug-like properties, Hit assessment and prioritization, Lead Optimization: fine tuning and risk mitigation, and more.
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Table of Contents
1. Risk Management in Early Discovery Medicinal Chemistry Gurpreet Singh, Jayme L. Dahlin and Michael A. Walters 2. Target Identification Using Chemical Probes Moses Moustakim, Suet Ling Felce, Nancy Zaarour, Gillian Farnie, Fiona E. McCann and Paul E. Brennan 3. Mining the Microbiome for Drug Targets Qi Wang, Fangming Yang and Huijue Jia 4. Screening Library Design Stephanie Kay Ashenden 5. Design of a Fragment Screening Library Ashley Taylor, Bradley C. Doak and Martin J. Scanlon 6. Genetically Encoded Cyclic Peptide Libraries: From Hit to Lead and Beyond Jacob Valentine and Ali Tavassoli 7. A Guide to Run Affinity Screens Using Differential Scanning Fluorimetry and Surface Plasmon Resonance Assays Christian Bergsdorf and Kirk Wright 8. Second-Harmonic Generation (SHG) for Conformational Measurements: Assay Development, Optimization, and Screening Tracy A. Young, Ben Moree, Margaret T. Butko, Bason Clancy, Mary Geck Do, Tarun Gheyi, John Strelow, Juan J. Carrillo and Joshua Salafsky 9. An Array-Based Ligand Discovery Platform for Proteins With Short Half-Lives Becky S. Leifer, Shelby K. Doyle, André Richters, Helen L. Evans and Angela N. Koehler 10. High Content, Phenotypic Assays and Screens for Compounds Modulating Cellular Processes in Primary Neurons Miklos Kepiro, Boglarka H. Varkuti and Ronald L. Davis 11. Achieving a Good Crystal System for Crystallographic X-Ray Fragment Screening Patrick M. Collins, Alice Douangamath, Romain Talon, Alexandre Dias, Jose Brandao-Neto, Tobias Krojer and Frank von Delft 12. Hit-to-Lead: Hit Validation and Assessment Kirk E. Hevener, JinHong Ren, Russell Pesavento, Kiira Ratia, Hyun Lee and Michael E. Johnson 13. Knowledge-Based Approaches to Off-Target Screening Daniel R. McMasters