In vitro screening technologies for VGSC drug discovery.
Assay type | Representative example | Temporal resolution | Information content | Throughput |
---|---|---|---|---|
Binding | Radioligand binding assay | Low (h) | Low (not functional) | Mid–high |
Ion flux | Radioisotope influx assay | Mid (s to min) | Mid | Mid–high |
AAS for Li+, Tl+ | ||||
Fluorescence dye | FLIPR membrane potential assay | Mid (s) | Mid | High |
FRET-based membrane potential assay (e.g., VIPR) | High (ms to s) | Mid | High | |
Electrophysiology | Automated patch-clamp assay | High (μs to ms) | High | Mid–high |
Manual patch-clamp assay | High (μs to ms) | High | Low |