Table 1. SAR exploration around compound 11.
| |||
Compound | R | clog P (log D) | Nav1.3 IC50 (nM) |
11 | 3.8 (3.3) | 17 | |
12 | 3.5 (2.5) | 147 | |
13 | 2.6 (1.8) | 2506 | |
14 | 3.7 (ND) | 155 | |
15 | 3.2 (ND) | 160 | |
16 | 4.1 (ND) | 45 | |
17 | 3.6 (ND) | 124 | |
18 | 2.9 (ND) | 3790 | |
19 | 2.6 (ND) | 4450 | |
20 | 4.0 (2.6) | 197 | |
21 | 4.3 (3.1) | 20 | |
22 | 4.5 (3.3) | 11 |