Book contents
- Frontmatter
- Contents
- Contributors
- Preface
- Section one Overviews
- Section two Molecules for Chemical Genomics
- Section Three Basics of High-Throughput Screening
- Section Four Chemical Genomics Assays and Screens
- Chapter 12 Basics of HTS Assay Design and Optimization
- Chapter 13 Molecular Sensors for Transcriptional and Post-Transcriptional Assays
- Chapter 14 Time-Resolved Fluorescence Resonance Energy Transfer Technologies in HTS
- Chapter 15 Compound Profiling with High-Content Screening Methodology
- Chapter 16 Use of Transgenic Zebrafish in a Phenotypic Screen for Angiogenesis Inhibitors
- Chapter 17 Flow Cytometry Multiplexed Screening Methodologies
- Chapter 18 Label-Free Biosensor Technologies in Small Molecule Modulator Discovery
- Chapter 19 Basic Principles and Practices of Computer-Aided Drug Design
- Chapter 20 Computational Approach for Drug Target Identification
- Section five Chemical Genomics and Medicine
- Index
- References
Chapter 15 - Compound Profiling with High-Content Screening Methodology
from Section Four - Chemical Genomics Assays and Screens
Published online by Cambridge University Press: 05 June 2012
- Frontmatter
- Contents
- Contributors
- Preface
- Section one Overviews
- Section two Molecules for Chemical Genomics
- Section Three Basics of High-Throughput Screening
- Section Four Chemical Genomics Assays and Screens
- Chapter 12 Basics of HTS Assay Design and Optimization
- Chapter 13 Molecular Sensors for Transcriptional and Post-Transcriptional Assays
- Chapter 14 Time-Resolved Fluorescence Resonance Energy Transfer Technologies in HTS
- Chapter 15 Compound Profiling with High-Content Screening Methodology
- Chapter 16 Use of Transgenic Zebrafish in a Phenotypic Screen for Angiogenesis Inhibitors
- Chapter 17 Flow Cytometry Multiplexed Screening Methodologies
- Chapter 18 Label-Free Biosensor Technologies in Small Molecule Modulator Discovery
- Chapter 19 Basic Principles and Practices of Computer-Aided Drug Design
- Chapter 20 Computational Approach for Drug Target Identification
- Section five Chemical Genomics and Medicine
- Index
- References
Summary
Over the last decades, high-throughput screening (HTS) of small molecule libraries has developed into a very powerful tool for drug discovery. Although HTS capabilities initially were developed almost exclusively in the domain of pharmaceutical and biotech commercial ventures, they have more recently become available in academia. The Molecular Library Initiative of the National Institutes of Health (NIH) is one example that HTS has established itself as a routine technology in biomedical research [1].
The popularity of HTS is due to rapid developments in four different areas:
Robotic systems. Once exotic and expensive, robotic systems and automatic liquid handling have become more affordable and easier to operate. Turnkey systems are available for the most common applications.
Chemical libraries. Chemical libraries are becoming more readily available and affordable to the scientific community in academia and industry. Even large compound libraries, such as the one developed for the above-mentioned Molecular Library Initiative, are accessible to the general scientific community.
Plate reader platforms. Reader platforms have undergone rapid development over the last two decades. As of today, high-speed microplate readers are available to very rapidly scan microplates in the 96-, 384-, and 1536-well formats or even higher densities. Automated confocal and conventional microscopes and other image-based reader platforms have evolved at an astonishing speed. Sophisticated image-based readers and corresponding image recognition and analysis software have led to the development of complex, high-content cell-based assays.
Detection technologies. A whole array of luminescence-based technologies have been developed and commercialized over the last few years. Among those are fluorescent proteins, high-yield fluorochromes, and luminescence substrates.
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- Chapter
- Information
- Chemical Genomics , pp. 215 - 224Publisher: Cambridge University PressPrint publication year: 2012