Table 1. Initial examination of C-6 amine SAR.
| ||||
R2 | TYK2 JH2 (IC50, μM) | TYK2/JAK1/JAK2 JH1 (IC50, μM) | IL23/IFNα (IC50, μM) | |
7 | 0.48 | >50 | 8.6/12.6 | |
10 | 0.032 | >2 | 1.1/1.5 | |
11 | 0.022 | >50/>2/>50 | 0.7/1.4 | |
12 | 0.024 | >2 | 1.4/1.7 | |
13 | 0.22 | >2 | 3.4/3.2 |