Table 2.
Results of a screen for a number of compounds with varying ion-channel blocking profiles. These screens were performed once for each ion channel at AZ. Where 50% block was not achieved, we have performed a least-squares fit of a concentration-effect curve to the original data, with a minimum allowed pIC50 of 0, a minimum allowed Hill coefficient of 0.5, and a maximum of 5.00.
Compound | hERG |
NaV1.5 |
CaV1.2 |
KCNQ1/minK |
Kv4.3/KChIP2.2 |
|||||
---|---|---|---|---|---|---|---|---|---|---|
pIC50 | Hill | pIC50 | Hill | pIC50 | Hill | pIC50 | Hill | pIC50 | Hill | |
Alfuzosin | 4.66 | 0.92 | 3.69 | 0.71 | 3.75 | 1.64 | 3.95 | 0.50 | 3.04 | 0.50 |
Dofetilide | 6.85 | 1.88 | 3.46 | 0.79 | 3.77 | 5.00 | 3.65 | 0.50 | 0.00 | 1.00 |
Lacosamide | 0.00 | 1.00 | 3.34 | 0.72 | 4.33 | 0.44 | 3.62 | 0.50 | 0.00 | 1.00 |
Nilotinib | 4.20 | 0.53 | 2.97 | 0.71 | 3.67 | 0.67 | 3.39 | 0.50 | 2.48 | 0.72 |
Tolterodine | 6.89 | 1.58 | 5.24 | 1.08 | 0.00 | 1.00 | 4.10 | 0.60 | 4.93 | 1.07 |