VU0477573 in vitro activity on rat mGlu5 in functional assays and radioligand binding
| Compound | Ca assay % Glut Max | Ca assay pIC50 | Ca assay IC50 | Binding pKi | Binding Ki |
|---|---|---|---|---|---|
| VU0477573a | ±S.E.M. | ±S.E.M. | nM | ±S.E.M. | nM |
| 16.43 ± 6.20 | 7.49 ± 0.16 | 32 | 7.85 ± 0.06 | 14 | |
| MPEP | −1.56 ± 0.89 | 7.87 ± 0.23 | 13 | 8.19 ± 0.03 | 6 |
| MTEP | −3.11 ± 1.26 | 7.28 ± 0.15 | 52 | 7.65 ± 0.03 | 22 |
↵a The operational model of allosterism parameters for negative allosteric modulation of glutamate-mediated intracellular calcium mobilization in HEK293A-rat-mGlu5-low cells by VU0477573 are logτA = 0.57 ± 0.13, pKB = 7.73 ± 0.10, logβ = -0.44 ± 0.10.