Table 3. Further In Vitro Characterization of VU6043653 (21iA).
| Metabotropic Glutamate Selectivity | ||
|---|---|---|
| IC50 (nM) | [%GluMin] | |
| human mGlu1a | inactive | |
| human mGlu2b | inactive | |
| human mGlu3b | >10,000 | [58] |
| human mGlu4a | inactive | |
| human mGlu7a | inactive | |
| human mGlu8a | inactive | |
| P450 Inhibition IC50 (μM)c | |||
|---|---|---|---|
| 1A2 | 2D6 | 2C9 | 3A4 |
| >30 | >30 | >30 | >30 |
a
Calcium mobilization assay.
b
G-protein-gated inwardly rectifying potassium channel (GIRK) assay.
c
Assay performed in pooled human liver microsomes (HLM) in the presence of NADPH with CYP-specific probe substrates.