Table 4. Off-Target Activity Data for the Selected Molecules.
% activity
at 1.0 × 10–6 Ma |
||||
---|---|---|---|---|
compd | H1R (%) | α1R (%) | M1R (%) | hERGb (%) |
2 | 39 | 48 | –15 | 23 |
3 | 58 | 66 | 5 | 34 |
5 | 54 | 39 | 4 | 31 |
7 | 29 | 56 | –7 | 28 |
11 | 24 | 43 | –5 | 29 |
15 | 10 | 13 | 11 | 29 |
16 | 2 | 14 | –1 | 40 |
18 | 19 | 19 | 7 | 38 |
21 | 4 | 15 | –6 | 47 |
Phentolamine | 91 | 76 | ||
Mepyramine | 95 | 55 | ||
Amitriptyline | 99 | 82 | 78 | |
Doxepin | 97 | 92 | ||
Quetiapine | 76 | 75 | 88 | |
Olanzapine | 89 | 82 | 89 | |
Verapamil | 91 |
% inhibition of control specific binding at the concentration of 1.0 × 10–6 M. Assays carried out in duplicate (n = 2). Blank spaces—compounds not tested in the assay.
% inhibition of hERG-mediated potassium currents at a concentration of 1.0 × 10–6 M.