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A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
Published on: March 10, 2017
Back to basics: label-free technologies for small molecule screening
Andrew K Shiau1, Mark E Massari, Can C Ozbal
1Department of Biology, Kalypsys Inc., San Diego, CA 92121, USA. ashiau@kalypsys.com
Combinatorial Chemistry & High Throughput Screening
|March 14, 2008
Summary
Label-free screening methods offer advantages over traditional assays in drug discovery by enabling the study of native biological systems. Recent technological advancements are enhancing their throughput for primary screening of compound libraries.
Area of Science:
- Biochemistry
- Drug Discovery
- Assay Development
Background:
- Current drug discovery screening relies heavily on labeled techniques, which can introduce experimental limitations.
- Label-free methods offer a way to study biological systems without artificial modifications, but have faced throughput and cost challenges.
Purpose of the Study:
- To review recent advancements in label-free screening technologies.
- To highlight how these improvements are increasing the utility of label-free methods for primary drug screening.
Main Methods:
- Review of recent improvements in impedance-based assays.
- Review of recent improvements in optical biosensor-based assays.
- Review of recent improvements in automated patch clamp technology.
- Review of recent improvements in mass spectrometry.
Main Results:
- Technological enhancements have improved the ease of use and throughput of label-free methods.
- These improvements position label-free techniques for primary screening of small- to medium-sized compound libraries.
- Advancements enable screening against minimally manipulated biological systems.
Conclusions:
- Label-free screening technologies are maturing and becoming more viable for primary drug discovery.
- Further development will allow for large-scale screening of chemical libraries using native biological systems.

