Handbook of Assay Development in Drug Discovery: 1st Edition (Hardback) book cover

Handbook of Assay Development in Drug Discovery

1st Edition

Edited by Lisa K. Minor

CRC Press

488 pages | 226 B/W Illus.

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Hardback: 9781574444711
pub: 2006-01-20
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The need to screen targets faster and more efficiently, coupled with advances in parallel and multiplex chemical synthesis, has contributed to the increasing use of multiwell assays for drug discovery. The Handbook of Assay Development in Drug Discovery is a reference that describes the complete armament of tools currently available for performing various assay techniques.

Featuring contributions from assay developers in the pharmaceutical and vendor communities, the book presents descriptions of methods, laboratory guidelines and protocols used to perform such methods, specific examples of each assay system, and troubleshooting tools. The handbook describes biochemical assay classes as well as non-class specific assay development for cell-based assays. It covers a wide range of target classes—including kinases, proteases, nuclear receptors, and GPCRs—and describes currently employed methods and assay types, such as radioligand binding assays, image analysis assays, enzyme fragment complementation, and bioluminescent and fluorescent-based assays.

Designed as a guide to running an assay from start to finish, the Handbook of Assay Development in Drug Discovery is an ideal bench top companion for discovery researchers, laboratory managers, academics, and other scientists involved in drug discovery screening, lead profiling, therapeutic target evaluation, and assay development and implementation in the pharmaceutical and biotechnology industries.

Daniel E. Levy, editor of the Drug Discovery Series, is the founder of DEL BioPharma, a consulting service for drug discovery programs. He also maintains a blog that explores organic chemistry.


“To be as advanced as possible, Dr. Minor has had individual chapters written by experts from equipment vendors (GE, PerkinElmer); pharmaceutical companies (J&J, Merck, Lilly), government (NIH) and more. These individual chapters describe in practical terms what these organizations have developed.”


Table of Contents

Protein Kinases in Drug Discovery: Rationale, Success, and Challenge; Dana L. Johnson and Jan L. Sechler

An Introduction to the Protein Tyrosine Phosphatase Gene Family and Screening Assay Development; Dominique Perrin and Rob Hooft van Huijsduijnen

Time-Resolved Fluorescence Based Assays for Kinases; Zhuyin Li and Tina Garyantes

Development of High-throughput Screening Assays in Scintillating Microplates (FlashPlates) to Identify Inhibitors of Kinase Activity; Stewart Emanual

Development of High-Throughput Screening Assays for Kinase Drug Targets using AlphaScreen™ Technology; D. Wenham, C. Illy, J.A. St. Pierre, and N. Bouchard

Homogeneous High-Throughput Screening (HTS) Assays for Serine/Threonine Kinases Using ß-Galactosidase Enzyme Fragment Complementation; I. Vainshtein, T. Naqvi, A. Lim, R. Rouhani, L. Kauffman, R. Singh, and R.M. Eglen

IMAP Assays for Assaying Protein Kinases; R. Sportsman

A Homogenous, Luminescent, High-Throughput, Versatile Assay for a Wide Range of Kinases; S.A. Goueli, K. Hsiao, and B. Bulleit

Proteases as Drug Targets; R.L. Thurmond and J.P. Edwards

A Comparison of Homogeneous Bioluminescent and Fluorescent Methods for Protease Assays; M. O’Brien

Scintillation Proximity Assay (SPA) Receptor Binding Assays; J.R. Cook, R. Graves, K. Lowitz, M.J. Price-Jones, J.A. Berry and K.T. Hughes

Radioligand Binding Filtration Assay: Full Automation; S.K.F. Wong

Nuclear Receptors As Drug Targets; P.D. Pelton

Nuclear Receptor Scintillation Proximity Assays; D. Powell and M.J. Price-Jones

Homogenous Assay Development for Nuclear Receptor Using the AlphaScreen Technology; N. Rouleau and R. Bossé

Development of Nuclear Receptor Homogenous Assay Using the Lance Technology; N. Rouleau, P. Hurskainen, I. Hemmilä and R. Bossé

The Emerging Role of Cell-based Assays in Discovery; R. Garippa

The Preparation of Cells for High-Content Screening; A. Hoffman

The Evolution of cAMP Assays; P. Kasila and H. Harney

A Homogenous Fluorescent Polariaiton assay for Inositol 1,4,5-Trisphoshpate (Ins P3); P. Fung, R. Singh, L. Kauffman, R.M. Eglen and T. Naqvi

Scintillation Proximity Assay of Inositol Phosphates; W. Zheng and P. Brandish

Measuring Calcium Mobilization with Gq-Coupled GPCRs Using the Fluorometric Imaging Plate Reader (FLIPR); J. Dunlop, Y. Zhang, R. Ring and D. Kowal

Development of FLIPR-Based HTS Assay for Gi-Coupled GPCRs; C. Chen, C. Smith, L. Minor, and B. Damiano

Aurora Assays; P, Kunapuli

Membrane Potential Based Assays for Ion Channels and Electrogenic Transporters; Q, Lü, S, Lin, and J, Dunlop

Reporter Gene Assays for Drug Discovery; K.A. Houck, W.P. Bocchinfuso, M.S. Dowless, and K.M. Borchert

mRNA Detection from Cells Using Quantigene® Branched DNA Technology; L. Minor

Homogeneous Miltiwell Assays for Measuring Cell Viability, Cytotoxicity and Apoptosis; Terry Riss, R.A. Moravec, M.A. O’Brien, E.M. Hawkins, and A. Niles

Development of Image-Bases Assays for Drug Discovery; S.M. Catalano

GPCR Internalization Measured by Image Analysis; R. Graves, M.J. Francis, L. Smith, J.R. Cook, and E.J. Adie

TRANSFLUOR®, a Universal Cell-Based Assay for Screening G-Protein Coupled Receptors; R. Oakley C.L. Cowan, C.C. Hudson, and C.R. Loomis

About the Series

Drug Discovery Series

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Subject Categories

BISAC Subject Codes/Headings:
MEDICAL / Pharmacy
SCIENCE / Chemistry / General
SCIENCE / Life Sciences / Genetics & Genomics