TABLE 3
Chemical optimization of VU0092273
| Compound |  | X | Y | Potency (EC50) | Efficacy | Ki |
|---|---|---|---|---|---|---|
| nM | % Glu Max | nM | ||||
| VU0092273 |  | H | CH | 10 ± 5 | 72 ± 7 | 970 ± 140 |
| VU0366025 |  | H | CH | 98 ± 4 | 90 ± 9 | 1480 ± 100 |
| VU0366026 |  | 3-F | CH | 5.2 ± 1.7 | 84 ± 3 | 1120 ± 170 |
| VU0366024 |  | H | CH | 19 ± 6 | 72 ± 11 | 1530 ± 320 |
| VU0240381 |  | H | CH | 2.3 ± 1.0 | 84 ± 8 | 55 ± 4 |
| VU0361747 |  | 3-F | N | 214 ± 89 | 107 ± 8 | N.D. |