Table 2.
Off-target binding of ITI-214 to a 70-substrate side effect profile diversity panel (General SEP II) was conducted by Caliper Life Sciences (PerkinElmer) using a single drug concentration of 10 μM ITI-214, a concentration that is ~300,000-fold in excess of the K i for PDE1 enzyme. A significant binding interaction in the assay was defined as >50 % binding to the target. The ten highest off-target binding interactions are shown in the table
| Specificity profile for ITI-214—20 highest off-target interactions | |
|---|---|
| Target | % Binding |
| Na+ channel (site 2), sodium channel | 88.44 |
| Ca2+ channel (L, DHP site) | 73.28 |
| NK3 (h), neurokinin | 64.65 |
| DA transporter (h), dopamine | 58.70 |
| Alpha 1 (non-selective), adrenergic | 40.90 |
| Potassium channel I[Kr], (hERG) | 35.09 |
| Alpha 2 (non-selective), adrenergic | 34.94 |
| H3 (h), histamine | 32.54 |
| NK1 (h), neurokinin | 30.93 |
| B2 (H), bradykinin | 30.79 |
h human, DHP dihydropyridine, hERG human ether-à-go-go-related gene