Table 2.
In Vitro Potency and Efficacy Data of Amide and Triazole-Containing Potentiators in the VX-770 Chemical Series in CFBE41o− and FRT Cells.[a]
| EC50 (nM)[b] | Maximal Response[c] | |||||||
|---|---|---|---|---|---|---|---|---|
| compd | WT CFBE | F508del CFBE | G551D CFBE | G551D FRT | WT CFBE | F508del CFBE | G551D CFBE | G551D FRT |
| VX-770 | 36.5 ± 21.3 | 1889 ± 1388 | 77.7 ± 27.2 | 428.5 ± 167.3 | 100.0% | 100.0% | 100.0% | 100.0% |
| 36 | -- | -- | 26.7± 79.4 | -- | Inactived | Inactived | 63.5% | Inactived |
| 37 | 21.8 ± 41.2 | 37.1 ± 48.2 | 18.5 ± 23.4 | 81.45 ± 102.8 | 47.5% | 36.3% | 72.0% | 36.7% |
| 56 | Inactive across all cell and CFTR typesd | |||||||
| 58 | Inactive across all cell and CFTR typesd | |||||||
| 60 | Inactive across all cell and CFTR typesd | |||||||
CFBE41o− abbreviated as CFBE.
Mean and standard deviation values from at least three determinations are reported.
Maximal response is reported as % activity of the VX-770 response.
No statistically significant response above DMSO vehicle.