Table 3. SAR of Indole N-1 and C-3 Positions.
| compd | R1 | R2 | TLR7 IC50 (nM)a | TLR9 IC50 (nM)a |
|---|---|---|---|---|
| 5n | H | Me | 250 ± 160 | 430 ± 260 |
| 7a | Me | Me | 5260 ± 1540 | 740 ± 170 |
| 7b | H | Cl | 1880 ± 710 | 430 ± 170 |
| 7c | H | CN | >10 000 | 260 ± 200 |
| 7d | H | CH2CH3 | 130 ± 100 | 490 ± 370 |
| 7e | H | CH2CF3 | 70 ± 40 | 750 ± 270 |
| 7f | H | isopropyl | 10 ± 7 | 700 ± 390 |
| 7g | H | isobutyl | 1290 ± 770 | 830 ± 770 |
IC50 values are a mean of two or more individual determinations.
