Table 4.
| |||||
---|---|---|---|---|---|
Cmpd | R1 | R2 | mGlu5 EC50 (nM)a | % Glu Maxb | Category |
11a | H | H | 5.9 | 104 | Ago-PAM |
11b | H | 870 | 40 | PAM | |
11c | H | 900 | 76 | PAM | |
11d | H | 5,700 | 44 | pAM | |
11e | H | m-F | 35 | 99 | Ago-PAM |
11f | H | m-F, p-F | 170 | 84 | PAM |
11g | H | p-F | 160 | 88 | PAM |
11h | H | o-F | 12 | 93 | Ago-PAM |
EC50s are the average of three determinations and are reproducible with a coefficient of variation of 0.3.
Determined at 30 μM test compound wherein %max vehicle is 10-30%.