Table 1. Summary of K2P Response to BL-1249a.
| background | mutant | EC50 (μM) | n (≥) |
|---|---|---|---|
| K2P2.1(TREK-1) | 5.5 ± 1.2 | 3 | |
| K2P2.1(TREK-1)GGG | 19 ± 1 | 3 | |
| K2P2.1(TREK-1)Δ322 | 26 ± 8b | 2 | |
| K2P2.1(TREK-1)Δ308 | 35 ± 8b | 2 | |
| TREK-1/AAK_T | 7.7 ± 0.6 | 2 | |
| TREK-1/AAK M4-C | 19 ± 3 | 3 | |
| TREK-1/AAK M3-C | 28 ± 2 | 3 | |
| TREK-1/AAK M2-C | 39 ± 9 | 3 | |
| TREK-1/TRAAK M2 | 26 ± 8 | 3 | |
| F172M | 15 ± 2 | 3 | |
| F185L | 27 ± 5 | 3 | |
| K2P10.1(TREK-2) | 8.0 ± 0.8 | 3 | |
| K2P4.1(TRAAK) | 48 ± 10b | 3 | |
| TRAAK/EK-1_T | 23 ± 4 | 2 | |
| TRAAK/EK-1 M4-C | 45 ± 2 | 3 | |
| TRAAK/EK-1 M3-C | 18 ± 2 | 3 | |
| TRAAK/EK-1 M2-C | 28 ± 5 | 3 | |
| TRAAK/TREK-1 M2 | 43 ± 11 | 3 | |
| M134F | 58 ± 34b | 2 | |
| L147F | 27 ± 4 | 3 |
a
Data derived from at least two independent experiments with each data point averaged from at least three oocytes.
b
Experiments where complete saturation of the response could not be reached due to BL-1249 solubility limits. For these cases, fits were imposed with an upper boundary of 15 (fold activation, I/I0) to estimate EC50 and error.