Table 2.
Pendant Aryl SAR of Bicyclic PAMs 9i-t.
| ||||
|---|---|---|---|---|
| Cmpd | R2 | mGlu5 EC50 (nM)a | % Glu Maxb | Category |
| 9j | o-CH3 | 610 | 53 | PAM |
| 9k | m-CH3 | 170 | 76 | Ago-PA |
| 9l | p-F | 260 | 81 | PAM |
| 9m | o-F | 150 | 80 | Ago-PA |
| 9n | p-CH3O | >10,000 | ND | ND |
| 9o | m-CH3O | 3,400 | 58 | PAM |
| 9p | m-CH3, p-F | 4,900 | 53 | PAM |
| 9q | o-CI | 3,700 | 50 | PAM |
| 9r | p-CI | >10,000 | ND | ND |
| 9s | m-CI | 470 | 68 | PAM |
| 9t | p-F, o-F | 850 | 59 | PAM |
a
EC50s are the average of three determinations and are reproducible with a coefficient of variation of 0.3.
b
Determined at 30 μM test compound wherein %max vehicle is 10-30%.