Flux assays in high throughput screening of ion channels in drug discovery
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Updated: Aug 24, 2026
High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
Sikander Gill1, Raj Gill, Soo Sen Lee
1Aurora Biomed Inc, Vancouver, BC, Canada. gill@aurorabiomed.com
Abstract:
Ion channels have been identified as therapeutic targets in various disorders, such as cardiovascular disease, neurological disease, and cystic fibrosis. Flux assays to detect functional ionic flux through ion channels are becoming increasingly popular as tools for screening compounds. In an optimized flux assay, modulation of ion channel activity may produce readily detectable changes in radiolabeled or nonradiolabeled ionic flux. Technologies based on flux assays are currently available in a fully automated high throughput format for efficient screening. This application offers sensitive, precise, and reproducible measurements giving accurate drug rank orders matching those of patch clamp data. Conveniently, the flux assay is amenable to adaptation for different ion channels, such as potassium, sodium, calcium, and chloride channels, by using suitable tracer ions. The nonradiolabeled rubidium-based flux assay coupled with the ion channel reader (ICR) technology has become very successful in ion channel activity analysis and is emerging as a popular technique in modern drug discovery.
Insights
Flux assays are effective tools for screening drug compounds targeting ion channels. The rubidium-based flux assay with ion channel reader (ICR) technology provides accurate, reproducible results for drug discovery.
Area of Science:
- Biochemistry
- Pharmacology
- Molecular Biology
Background:
- Ion channels are crucial therapeutic targets for diseases like cardiovascular and neurological disorders.
- Flux assays are increasingly utilized for screening compounds that modulate ion channel activity.
Purpose of the Study:
- To highlight the utility of flux assays in ion channel research.
- To present the rubidium-based flux assay and ion channel reader (ICR) technology as a successful drug discovery tool.
Main Methods:
- Utilizing optimized flux assays to detect functional ionic flux.
- Employing radiolabeled or nonradiolabeled tracers for flux measurement.
- Adapting flux assays for various ion channels (potassium, sodium, calcium, chloride) using specific tracer ions.
Main Results:
- Flux assays provide sensitive, precise, and reproducible measurements.
- High-throughput, automated flux assay technologies enable efficient screening.
- The nonradiolabeled rubidium-based flux assay with ICR technology demonstrates high success in ion channel analysis.
Conclusions:
- Flux assays are valuable, adaptable tools for ion channel drug discovery.
- The rubidium-based flux assay coupled with ICR technology is a popular and effective modern drug discovery technique.
