Ion Channels Assays

Ion channels regulate a wide range of physiological processes including rapid electrical signaling, fluid, hormone and transmitter secretion, and proliferation. Ion channel screening assays applying traditional and high throughput screening (HTS) technologies have been utilized for drug R&D. HTS methods for ion channels include: the ligand binding assay, flux-based assay, fluorescence-based assay and automated electrophysiological assay.

Figure 1 Ion Channels

Ligand Binding Assays

• Detect the binding affinity of a compound to an ion channel using conventional instrumentation. Throughput represents its major strength.

Flux-Based Assays

• Directly access a functional change of ion channel activity.
• A nonradioactive Rb⁺ efflux assay was developed that uses atomic absorption spectroscopy to detect rubidium.

Fluorescence-Based Assays

• Measure either the membrane-potential-dependent or ion-concentration-dependent changes of fluorescence signals as a result of ionic flux.
• Produce a robust and homogeneous cell population measurement.
• Easy to implement and to optimize to achieve a higher throughput.
• Different ion-specific synthesized fluorescent probes have been developed.
• Fluorescent voltage-sensitive dyes measure voltage changes across the cellular membrane using either the potential-dependent accumulation and redistribution, or the fluorescence resonance energy transfer (FRET) mechanism.

Automated Electrophysiological Assays

• Provide a giga-ohm seal quality of data comparable to a manual electrophysiology recording.
• Rely on the use of a perforated patch clamp technique with higher throughput.
• Not compromise data quality and pharmacology.

Our Ion Channel Screening Services

• Computational chemistry for knowledge-based compound deck selection from our diverse compound library.
• Assay development and transfer services to compliment your current study design.
• Ion channel selectivity profiling.
• Hit-to-lead and lead optimization support.

The development of ion channel screening technologies has met most needs for drug discovery. In order to successfully implement improved ion channel screening assays that provide pharmacologically relevant data, it is critical to carefully evaluate and control a variety of assay parameters. Our scientists in CD ComputaBio can advise on the best high-throughput screening (HTS) approach for your ion channel assay, for screening and profiling ion channel targets, including major cardiac, central nervous system (CNS), and peripheral nervous system (PNS) channels.