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. Author manuscript; available in PMC: 2020 Mar 7.
Published in final edited form as: Chemistry. 2019 Feb 11;25(14):3662–3674. doi: 10.1002/chem.201805919

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
a

CFBE41o abbreviated as CFBE.

b

Mean and standard deviation values from at least three determinations are reported.

c

Maximal response is reported as % activity of the VX-770 response.

d

No statistically significant response above DMSO vehicle.