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TLR signaling inhibition by pyrazoles with different C3 basic side chains.
 | |||||||
|---|---|---|---|---|---|---|---|
| Cmpd | R | BSC | IC50 (μM) | ||||
| TLR9 | TLR7 | TLR2 | TLR4 | Tox. | |||
| 72 | OH |  |
3.36 ± 0.09 | 4.62 ± 0.12 | 5.88 ± 0.31 | 6.11 ± 0.48 | 26.0 ± 0.5 |
| 73 | OMe |  |
3.42 ± 0.34 | 3.52 ± 0.03 | 12.8 ± 0.3 | n.d. | 8.69 ± 2.41 |
| 74 | OMe |  |
3.46 ± 0.18 | 5.55 ± 0.22 | n.d. | n.d. | 4.99 ± 1.70 |
| 75 | OMe |  |
> 50 | 2.27 ± 0.95 | > 50 | > 50 | > 50 |
n.d. = not determined
