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High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
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A robotic platform for quantitative high-throughput screening.

Sam Michael1, Douglas Auld, Carleen Klumpp

  • 1NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20850, USA.

Assay and Drug Development Technologies
|November 28, 2008
PubMed
Summary
This summary is machine-generated.

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Quantitative high-throughput screening (qHTS) utilizes automated systems to generate concentration-response curves for millions of compounds. This approach enhances efficiency and accelerates drug discovery in academic settings.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • High-throughput screening (HTS) adoption in academia presents unique challenges and opportunities.
  • Technological advancements enable automated, miniaturized screening in 1,536-well formats.
  • Quantitative HTS (qHTS) generates concentration-response curves (CRCs) for comprehensive data.

Purpose of the Study:

  • To describe the design and implementation of an automated screening system for qHTS.
  • To report on the system's productivity, reliability, and flexibility.
  • To detail modifications for increased throughput and expanded capabilities.

Main Methods:

  • Developed a fully integrated and automated screening system for qHTS.
  • Implemented miniaturization and high-efficiency protocols for cell-based and biochemical assays.

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Last Updated: Jun 27, 2026

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  • Tested libraries exceeding 100,000 compounds, generating millions of sample wells.

    • Main Results:

    • Generated over 6 million CRCs from more than 120 assays in three years.
    • Demonstrated high system productivity, reliability, and flexibility.
    • Successfully modified the system to enhance throughput and add capabilities.

    Conclusions:

    • The integrated automated system effectively supports qHTS for large-scale screening.
    • This technology can be widely implemented to improve screening efficiency and lead generation.
    • qHTS combined with automation offers a powerful paradigm for drug discovery.