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This volume presents both theoretical guidance and protocols on chemogenomics including chemogenomics library assembly, compound profiling, and phenotypic assays.
An Introduction to Chemogenomics.- Developing a Kinase Chemogenomic Set: Facilitating Investigation into Kinase Biology by Linking Phenotypes to Targets.- Compilation of Custom Compound/Bioactivity Datasets from Public Repositories.- Quality Control of Chemogenomic Library using LC-MS.- Annotation of the Effect of Chemogenomic Compounds on Cell Health using High-Content Microscopy in Live-Cell Mode.- Characterization of Cellular Viability using Label-Free Brightfield Live-Cell Imaging.- Plate-Based Screening for DUB Inhibitors.- NanoBRET™ Live Cell Kinase Selectivity Profiling Adapted for High Throughput Screening.- A Fluorescence-Based Reporter Gene Assay to Characterize Nuclear Receptor Modulators.- Measuring Protein-Protein Interactions in Cells using NanoLuciferase Bioluminescence Resonance Energy Transfer (NanoBRET) Assay.- HiBiT Cellular Thermal Shift Assay (HiBiT CETSA).- Detection of Cellular Target Engagement for Small Molecule Modulators of Striatal-Enriched Protein Tyrosine Phosphatase (STEP).- Target Deconvolution by Limited Proteolysis Coupled to Mass Spectrometry.- Global Assessment of Drug Target Engagement and Selectivity of Covalent Cysteine-Reactive Inhibitors using Alkyne-Functionalized Probes.- 3D-Spheroid Invasion Assay for High-Throughput Screening of Small Molecule Libraries.- Live-Cell High-Throughput Screen for Monitoring Autophagy Flux.- Phenotypic Chemical Screening in CD4+ T Cells to Identify Epigenetic Inhibitors.
