Pharmaceutical Book from C.H.I.P.S.

High Throughput-Screening in Drug Discovery
edited by Jörg Hüser

High Throughput-Screening in Drug Discovery is a professional guide to successful compound screening in pharmaceutical research and chemical biology.


  • Includes the chemoinformatic tools needed for correct data evaluation
  • Discusses such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results


Chemical Genetics: Use of High-throughput Screening to Identify Small-molecule Modulators of Proteins Involved in Cellular Pathways with the Aim of Uncovering Protein Function

  • Classical and Chemical Genetics
  • Identifying Bioactive Molecules
  • Target Identification
  • Discovery for Basic Research Versus Pharmacotherapy Goals
  • Chemical Genetic Screens in the Academic Setting

High-throughput Screening for Targeted Lead Discovery

  • Chemical Libraries for High-throughput Screening
  • Properties of Lead Structures
  • Challenges to High-throughput Screening
  • Assay Technologies for High-throughput Screening
  • Laboratory Automation
  • From Target Selection to Confirmed Hits – the HTS Workflow and its Vocabulary
  • Separating Specific Modulators from Off-Target Effects
  • Data Analysis and Screening Results

Tools and Technologies that Facilitate Automated Screening

  • Sample Carriers
  • Liquid Handling Tools
  • Detection Technologies
  • Laboratory Robotics

Functional Cell-based Assays for Targeted Lead Discovery in High-throughput Screening

  • Reporter Gene Technologies
  • Membrane Potential Indicators
  • Ca2+ Indicators

Biochemical Assays for High-throughput Screening

  • General Considerations for Biochemical High-throughput Screening
  • Expression and Purification of Recombinant Enzymes
  • Peptidases
  • Oxidoreductases
  • Transferases, Synthetases and Lipid-modifying Enzymes
  • Kinases
  • Pitfalls and Reasons for Assay Development Failures

Image-based High-content Screening – A View from Basic Sciences

  • HCS Systems Employing Confocal Optical Technologies
  • Single-point Scanning Technology
  • Line Scanning Technology
  • Multi-beam Technology
  • Structured Illumination
  • Summary and Perspectives

Methods for Statistical Analysis, Quality Assurance and Management of Primary High-throughput Screening Data

  • Statistical Considerations in Assay Development
  • Data Acquisition, Data Preprocessing, and HTS Data Analysis Environment
  • Data Normalization
  • Robust Statistics in HTS Data Analysis
  • Measures of HTS Data Quality, Signaling of Possible QC Problems, Visualizations
  • Correction of Position-dependent Response Effects
  • Hit Identification and Hit Scoring

Chemoinformatic Tools for High-throughput Screening Data Analysis

  • Workflow of High-throughput Screening and Use of Chemoinformatics
  • Chemoinformatic Methods Used in HTS Workflow
  • Chemoinformatic Methods in the Design of a Screening Library
  • Integrated Software Packages

Combinatorial Chemistry and High-throughput Screening

  • Categories of Compound Libraries for High-throughput Screening
  • Synthesis Techniques and Library Formats
  • Library Design and Profiling Approaches
  • Impact of Combinatorial Libraries on Drug Discovery

High-throughput Screening and Data Analysis

  • Analysis of Cellular Screening Data
  • Massively Parallel Cellular Screens
  • Systematic Serendipity


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High Throughput-Screening in Drug Discovery
edited by Jörg Hüser
2006 • 362 pages • $199.00 + shipping
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