Table 6.
Primary safety‐pharmacology panel of 24 and functional assessment of CEREP off‐targets of 24 (de‐risking)
| Assay target | IC50 [×10−6 m] | Assay method/note |
|---|---|---|
| hERG inhibition | 15.8 | Electrophysiology |
| fold AhR receptor induction | 0.91 @1 × 10−6 m a) | Luciferase reporter gene assay |
| CYP3A4 inhibition | >25 b) | Metabolic activity |
| CYP2D6 inhibition | >25 | Metabolic activity |
| CYP1A inhibition | >25 | Metabolic activity |
| CYP2C9 inhibition | >25 | Metabolic activity |
| CYP2C19 inhibition | >25 | Metabolic activity |
| Mini‐AMES | Negative @62.25 µg mL−1 (147 × 10−6 m) | |
|
Ca2+ channel inhibition, Cerep 161 |
>30 | Binding, antagonist |
|
Norepinephrine transporter, Cerep 355 |
>10 | Binding, antagonist |
|
5‐HT2B receptor, Cerep 1333 |
>10 | Binding, agonist |
|
Na+ channel, Cerep 169 |
>30 | Binding, antagonist |
a)
fold activation at given concentration
b)
activation observed.