Preface

Phenotypic drug discovery has been highlighted in the past decade as an important strategy in the discovery of novel medical entities. How many marketed drugs are actually derived from phenotypic screens? From the most recent examples, what were the factors enabling target identification and validation? What are the contemporary technology platforms required for successful application? It is our aim that by bringing together this volume we can equip researchers with an in-depth up-to-date knowledge of key approaches and criteria involved in successful delivery of clinical candidates from phenotypic screens, thus aiding in the utilisation of this strategy for medicines discovery.

The first chapter introduces readers to the history and evolution of phenotypic drug discovery. Chapters 2 to 7 of the book bring together chapters that discuss the fundamental capabilities required for phenotypic discovery. These chapters include the design and use of disease-relevant assays, perturbant libraries, target deconvolution and collaborative models for project execution. The focus of this section is on how new and emerging technologies are enabling a contemporary approach to phenotypic drug discovery. Chapters 8 to 13 bring together a collection of recent case studies in target-agnostic approaches for the identification of small and large molecules that have progressed into clinical development for a diverse array of disease indications. Such a collection has not until now been available to drug hunters. Chapters, written by experienced practitioners across academia and industry, explain the strategy and platforms used. Perspectives on key success factors, technologies and future directions are shared.

We would like to say a big thank-you to all the authors for their dedication to and participation in this project. We are grateful to the Royal Society of Chemistry Drug Discovery series editors; Ian Storer, Hong Shen, David Thurston, David Fox, Ana Martinez and David Rotella for their unwavering support and helpful input. Special thanks also to Katie Morrey and Liv Towers, editorial assistants at the Royal Society of Chemistry and to Drew Gwilliams, the commissioning editor at the Royal Society of Chemistry, without whom the book would not have been possible. Thanks to all for making this project such an enjoyable experience. Lastly, to you the reader, we hope you will find this volume both useful and entertaining.

Bev Isherwood and Angélique Augustin