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 wish had been available when they started in HTS, these expert 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.

Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharma and biotech industries working on small molecule screening.

High throughput screening remains a key part of early stage drug and tool compound discovery, and methods and technologies have seen many fundamental improvements and innovations over the past 20 years. This comprehensive book provides a historical survey of the field up to the current state-of-the-art. In addition to the specific methods, this book also considers cultural and organizational questions that represent opportunities for future success. Following thought-provoking foreword and introduction from Professor Stuart Schreiber and the editors, chapters from leading experts across academia and industry cover initial considerations for screening, methods appropriate for different goals in small molecule discovery, newer technologies that provide alternative approaches to traditional miniaturization procedures, and practical aspects such as cost and resourcing. Within the context of their historical development, authors explain common pitfalls and their solutions. This book will serve as both a practical reference and a thoughtful guide to the philosophy underlying technological change in such a fast-moving area for postgraduates and researchers in academia and industry, particularly in the areas of chemical biology, pharmacology, structural biology and assay development.

The development of suitable assays, the integration of appropriate technology, and the effective management of the essential infrastructure are all critical to the success of any high-throughput screening (HTS) endeavor. However, few scientists have the multidisciplinary experience needed to control all aspects of an HTS drug discovery project. A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery integrates the experience of diverse experts who offer fundamental and practical guidance across numerous situations. The book first discusses assay developments for important target classes such as protein kinases and phosphatases, proteases, nuclear receptors, G protein-coupled receptors, ion channels, and heat shock proteins. It next examines assay developments for cell viability, apoptosis, and infectious diseases. The contributors explore the application of emerging technologies and systems, including image-based high content screening, RNA interference, and primary cells. Finally, they discuss the essential components of the integrated HTS process, such as screening automation, compound library management, the screening of natural products from botanical sources, and screening informatics. Designed to motivate researchers to bring further advances to the field, this volume provides practical guidance on how to initiate, validate, optimize, and manage a bioassay intended to screen large collections of compounds. Drawing on the knowledge from experts actively involved in assay development and HTS, this is a resource that is both comprehensive and focused.

Furnishing the latest interdisciplinary information on the most important and frequently the only investigational system available for discovery programs that address the effects of small molecules on newly discovered enzyme and receptor targets emanating from molecular biology, this timely resource facilitates the transition from classical to high

The book focuses on various aspects and properties of high-throughput screening (HTS), which is of great importance in the development of novel drugs to treat communicable and non-communicable diseases. Chapters in this volume discuss HTS methodologies, resources, and technologies and highlight the significance of HTS in personalized and precision medicine.

The development of suitable assays, the integration of appropriate technology, and the effective management of the essential infrastructure are all critical to the success of any high-throughput screening (HTS) endeavor. However, few scientists have the multidisciplinary experience needed to control all aspects of an HTS drug discovery project. A P