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