Table 4. TLR Cellular and Whole Blood Activity Data for 7f.
| assay | receptor | IC50 (nM)a |
|---|---|---|
| HEK293; NF-kB reporter (antagonist mode) | TLR9 | 700 ± 390 |
| TLR8 | 17 ± 37 | |
| TLR7 | 10 ± 7 | |
| TLR4 | 15100 ± 16500 | |
| TLR3 | 5440 ± 5000 | |
| HEK293; NF-kB reporter (agonist mode) | TLR7,8,9 | >50000 |
| PBMCs; IL-6 | TLR9 | 510 ± 80 |
| TLR7 | 4.8 ± 3.6 | |
| pDC (ODN2216); IFNαpDC (flu virus); IFNα | TLR9 | 210 ± 390 |
| TLR7 | 11 ± 9 | |
| human whole blood; IL-6 | TLR9 | 320 ± 97 |
| TLR8 | 5.1 ± 5.6 | |
| TLR7 | 5.7 ± 6.3 | |
| mouse whole blood; IL-6 | TLR9 | 510 ± 150 |
| TLR7 | 43 ± 45 | |
a
IC50 values are a mean of two or more individual determinations. See Supporting Information for assay details.