Table 1 IC50s of Inh-172 and Hill coefficient values for all CFTR constructs
From: Allosteric inhibition of CFTR gating by CFTRinh-172 binding in the pore
Constructs Values | IC50 (µM) | Hill Coefficient |
|---|---|---|
Human WT | 0.08 ± 0.01 | 0.88 ± 0.09 |
K95A | 0.85 ± 0.05 | 0.98 ± 0.05 |
M348K | 0.52 ± 0.06 | 0.90 ± 0.10 |
T1142A | 0.27 ± 0.01 | 0.81 ± 0.02 |
T1142I | 1.49 ± 0.07 | 1.12 ± 0.05 |
W1145A | 0.88 ± 0.09 | 1.08 ± 0.12 |
W1145L | 0.64 ± 0.06 | 0.82 ± 0.07 |
W1145Y | 0.87 ± 0.03 | 0.92 ± 0.03 |
Pig WT | 1.86 ± 0.12 | 0.83 ± 0.04 |
h-pTMD1-h | 0.11 ± 0.01 | 0.98 ± 0.10 |
p-hTMD1-p | 2.21 ± 0.07 | 1.03 ± 0.03 |
h-pTMD2-h | 4.02 ± 0.28 | 0.69 ± 0.04 |
p-hTMD2-p | 0.06 ± 0.02 | 0.54 ± 0.08 |
h-pTM8-h | 0.64 ± 0.02 | 0.80 ± 0.02 |
p-hTM8-p | 0.72 ± 0.09 | 0.84 ± 0.10 |
Human WT + 200 nM VX-770 | 0.25 ± 0.02 | 1.07 ± 0.10 |
Human WT + 1 µM VX-770 | 0.42 ± 0.01 | 0.98 ± 0.02 |
