Anthony W. Czarnik

Few scientists have access to the multidisciplinary experience needed for successful assay development and high-throughput screening (HTS) in drug discovery. Designed to give researchers a boost, this text integrates the experience of diverse experts who offer fundamental practical guidance across numerous situations. It introduces emerging technology that allows scientists to identify and capture relevant information. It instructs in how to initiate, validate, optimize, and manage a bioassay intended to screen large collections of compounds. It also identifies critical targets of relevance in drug discovery and treats each individually in terms of the parameters needed for successful assay development.

High throughput analysis plays a critical role in the pharmaceutical industry. The ever-shortening timelines and high costs of drug discovery and development have brought about the need for high throughput approaches to methods that are currently used in the industry. Written and edited by well-known contributors who remain active in this line of research, this book systematically describes high throughput analysis for the pharmaceutical industry, including advanced instrumentation and automated sample preparation. The text discusses various techniques, including HPLC, MALDI-MS, and LC-MS/MS methods, with an emphasis on the later stage of drug development, including pharmacokinetics.

A single source on parallel synthesis for lead optimization, this book features real-world examples and contributions from well-known scientists. It explores the shift to conducting parallel lead optimization in-house while outsourcing most of the screening libraries synthesis. With more than 15 case studies that encompass a range of biological targets for application in different therapeutic areas, the text contains examples of solid and solution-phase techniques for the synthesis of directed libraries. The chapter authors explain the design principles they used to direct the choice of templates and diversity elements. They explore how this technology, when applied to library design, can speed up drug discovery.