Design and Implementation of High Throughput Screening Assays -- Configuring Radioligand Receptor Binding Assays for HTS Using Scintillation Proximity Assay Technology -- Homogeneous Techniques for Monitoring Receptor–Ligand Interactions -- Comparison of SPA, FRET, and FP for Kinase Assays -- Electrochemiluminescence: A Technology Evaluation and Assay Reformatting of the Stat6/P578 Protein–Peptide Interaction -- Cellular Assays in HTS -- Compound Library Management -- Compound Library Management: An Overview of an Automated System -- Natural Products or Not? How to Screen for Natural Products in the Emerging HTS Paradigm -- to Screening Automation -- Unit Automation in High Throughput Screening -- Fully Automated Screening Systems -- Management and Maintenance of High Throughput Screening Systems.

Since its first use in antibiotic research in the 1940s, High Throughput Screening (HTS) has evolved into a major enabling tool and methodology in the discovery of pharmaceutical, chemical, and agricultural compounds. In High Throughput Screening, leading scientists and researchers expert in molecular discovery explain the diverse technologies and key techniques used in HTS and demonstrate how they can be applied generically. Writing to create precisely the introductory guidebook they wished had been available when they started in HTS, these seasoned authors illuminate the HTS process with richly detailed tutorials on the biological techniques involved, the management of compound libraries, and the automation and engineering approaches needed. Extensive discussions provide readers with all those key elements of pharmacology, molecular biology, enzymology, and biochemistry that will ensure the identification of suitable targets and screens, and detail the technology necessary to mine millions of data points for meaningful knowledge. By presenting accounts not only of the basic principles underlying HTS technology, but also real-use cases, High Throughput Screening constitutes a highly practical introduction to HTS, even as it also provides sufficient detail to work more productively in today's lead generation laboratories.