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 12 - Basics of HTS Assay Design and Optimization
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
High-throughput screening (HTS) is a production process aimed at testing tens of thousands of compounds per hour for the identification of a small subset of compounds that display a desired property, such as affecting a biological target of interest. As with any production process, the output of HTS depends profoundly on the quality of input materials, assay reagents and chemical compound libraries, as well as on the reliability of the process itself, a major component of which is a biological assay employed for testing compounds.
The utility of HTS assays depends on the correlation between biological properties of model systems, macromolecules or cellular pathways, and measurable biophysical properties gauging the effect of screened compounds on the HTS target of interest. Compounds with desired properties, identified as actives or HTS hits, need to be unequivocally distinguished from “inactive” compounds. Because of the number of compounds simultaneously tested in HTS, screening assays must be extremely reproducible and robust to provide statistically reliable results. Furthermore, HTS assays must be fine-tuned to enhance their ability to distinguish hits with desired pharmacologic properties apart from all other compounds. Achieving these generic and specific traits of HTS assays is described in detail in this chapter.
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- Information
- Chemical Genomics , pp. 159 - 172Publisher: Cambridge University PressPrint publication year: 2012
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