Table 4.
| |||
|---|---|---|---|
| Compd | R1 | hmGlu4 EC50 (μM)a | % Inhibition |
| 5a |
|
Inactive | 12.0 ± 12.2 |
| 5b |
|
Inactive | −8.7 ± 4.2 |
| 5c |
|
Inactive | −10.7 ± 10.2 |
| 5d |
|
7.7 ± 0.8 | 58.5 ± 16.3 |
| 5e |
|
Inactive | −2.8 ± 5.0 |
| 5f |
|
Inactive | 4.4 ± 9.9 |
| 5g |
|
Inactive | 12.9 ± 13.2 |
| 5h |
|
Inactive | 16.9 ± 11.0 |
| 5i |
|
Inactive | −18.3 ± 12.0 |
| 5j |
|
4.7 ± 0.5 | 59.8 ± 14.6 |
| 5l |
|
Inactive | −17.0 ± 3.6 |
| 5m |
|
Inactive | −14.8 ± 8.7 |
| 5n |
|
>10 | 31.1 ± 15.8 |
| 5o |
|
8.0 ± 0.9 | 60.0 ± 9.4 |
| 5p |
|
Inactive | −3.4 ± 2.4 |
| 5q |
|
Inactive | −4.8 ± 6.4 |
| 5r |
|
Inactive | 7.8 ± 3.3 |
| 5s |
|
Inactive | 7.4 ± 5.2 |
| 5t |
|
>10 | 56.2 ± 12.7 |
| 5u |
|
Inactive | −10.4 ± 9.4 |
| 5v |
|
Inactive | −0.1 ± 4.6 |
| 5w |
|
>10 | 36.5 ± 13.7 |
| 5x |
|
Inactive | −7.1 ± 9.2 |
a
IC50 and % EC80 values are the average of at least three independent determinations performed in triplicate (mean ± SEM shown in table). Compounds were ranked as active if they inhibited the EC80 response by at least 20%.