TABLE 3.
Cooperativity estimates (logβ) for mGlu5 NAMs from functional assays
Collated data were fitted to the operational model of allosterism. Data represented as means ± S.E.M. from the indicated number (n) of independent experiments performed in triplicate.
| Ca2+ mobilization | IP1 accumulation | ERK1/2 phosphorylation | Receptor internalization | |||||
|---|---|---|---|---|---|---|---|---|
| logβ | n | logβ | n | logβ | n | logβ | n | |
| AZD2066 | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.30 ± 0.04 | 3 |
| Basimglurant | full NAM | 3 | full NAM | 4 | full NAM | 4 | −0.41 ± 0.06 | 3 |
| Dipraglurant | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.32 ± 0.04 | 3 |
| F169521 | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.44 ± 0.07 | 3 |
| F1699611 | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.28 ± 0.03 | 3 |
| Mavoglurant | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.26 ± 0.03 | 3 |
| Remeglurant | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.39 ± 0.05 | 3 |
| (RS)-remeglurant | full NAM | 3 | full NAM | 4 | −0.24 ± 0.04 | 3 | −0.41 ± 0.07 | 3 |
| STX107 | full NAM | 3 | full NAM | 4 | full NAM | 3 | −0.30 ± 0.05 | 3 |