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.
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.

Perspective/overview: State of the art in HTS at the academic-industry interface; Assay design and optimization; Assessment of available compound collections; Novel approaches to discovery and analysis of interesting compound combinations; Modern biophysical methods in target-based screening; Genetic perturbation methods; Understanding luminescence-based screens; Measuring interactions in live cells; Approaches to high-content imaging and multi-feature analysis; Profiling of genetically characterized cell systems; Multidimensional profile-based screening; Using biological systems that better recapitulate physiology; Phenotypic screens with model organisms; Encoded libraries; Modern virtual screening; Research data management; Small molecule bioactivity databases; Chemical biology in a pharma environment; Practical aspects of funding and executing high-throughput screens;