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Functional cell-based assays in microliter volumes for ultra-high throughput screening
Frank Wunder1, Bernd Kalthof, Thomas Müller
1Molecular Screening Technology, Bayer HealthCare AG, Bayer-Schering Pharma, Wuppertal, Germany.
Combinatorial Chemistry & High Throughput Screening
|August 13, 2008
Summary
Ultra-high throughput screening (uHTS) using cell-based assays in 1536-well plates enables rapid testing of millions of compounds. This approach supports drug discovery by integrating compound logistics, automated testing, and hit characterization for efficient identification of potential therapeutics.
Area of Science:
- Biochemistry
- Pharmacology
- Cell Biology
Background:
- Functional cell-based assays are crucial for microplate-based high throughput screening (HTS).
- High-density microplates (e.g., 1536-well) and miniaturized formats facilitate screening of large compound libraries (>1 million compounds) at ultra-high throughput (>100,000 samples/day).
- uHTS operations require efficient compound logistics, automated bioassays, and follow-up studies for hit confirmation and characterization.
Purpose of the Study:
- To review the feasibility and trends in cell-based ultra-high throughput screening (uHTS).
- To categorize cell-based assays based on response kinetics and readout methods.
- To highlight advancements in assay development for improved hit identification and characterization.
Main Methods:
- Categorization of cell-based assays by response kinetics (fast vs. transcriptional) and readout methods.
- Discussion of automation and robotic systems for complex assay protocols.
- Review of miniaturized assay formats in high-density microplates.
Main Results:
- Cell-based uHTS in microliter volumes is feasible with full automation.
- Assays range from measuring fast cellular responses (e.g., calcium signals) to transcriptional responses.
- Trends include incorporating assay reference signals and using kinetic, real-time readouts.
Conclusions:
- Cell-based uHTS is a powerful tool for screening large compound collections efficiently.
- Automation and advanced assay designs enhance the reliability and information content of screening campaigns.
- Future directions focus on differentiating target hits and understanding compound mode-of-action through kinetic analysis.
