Table 7.
Potency and selectivity of KV1.3 inhibitors identified in automated electrophysiological patch‐clamp assays
| Structural class | Compound | Cell type | Type of automated electrophysiological assay | IC50 (nM) or % inhibition | Selectivity over KV1.5 |
|---|---|---|---|---|---|
| Thienopyridines | 5 162 | CHO cells expressing KV1.3 | Automated pipette‐based patch‐clamp (autopatch electrophysiology method) | 1 µM: 99% inhibition | 1 µM: 93% inhibition |
| Sulfonamides | 6 163 | CHO cells expressing KV1.3 | Automated pipette‐based patch‐clamp (autopatch electrophysiology method) | 1 µM: 100% inhibition | 1 µM: 91% inhibition |
| 1,1‐[d]‐Dioxidobenzo isothiazoles | 7 164, 165 | CGE22 cells expressing human KV1.3 |
Micro‐fabricated planar electrode‐based patch clamp (ionWorks platform) |
1000 | Not studied |
| 7g 164, 165 | 350 | IC50 = 540 nM | |||
| 7h 164, 165 | 250 | IC50 = 480 nM | |||
| Amine derivates | 8 166 | CHO cells expressing KV1.3 | Planar electrode‐based patch clamp (Nanion Technologies) whole‐cell patch‐clamp | <50 | Not studied |