TABLE 4
Chemical optimization of VU0092273 combining optimal findings from each library
| Compound |  | X | Y | Potency (EC50) | Efficacy | Ki |
|---|---|---|---|---|---|---|
| nM | % Glu Max | nM | ||||
| VU0366030 |  | 3-F | CH | 23 ± 6 | 82 ± 8 | 1440 ± 150 |
| VU0366027 |  | 3-F | CH | 7.1 ± 2.1 | 72 ± 6 | 1580 ± 210 |
| VU0366031 |  | 3-F | CH | 3.8 ± 1.1 | 98 ± 8 | 40 ± 12 |
| VU0366028 |  | 3,4-difluoro | CH | 25 ± 5 | 103 ± 6 | 390 ± 50 |
| VU0366029 |  | 3-F | CH | 65 ± 16 | 104 ± 3 | 980 ± 20 |
| VU0360175 |  | 3-F | N | 49 ± 7 | 105 ± 4 | N.D. |
| VU0360172 |  | 3-F | N | 16 ± 6 | 87 ± 3 | 195 ± 20 |