Table 2. Optimization of C-8 amine.
| |||
R1 | TYK2 JH2 (IC50, μM) | IL23/IFNα (IC50, μM) | |
11 | 0.022 | 0.7/1.4 | |
18 | 0.007 | 0.1/0.05 | |
19 | 0.017 | 0.6/0.6 | |
20 | 0.11 | 6.2/4.1 | |
21 | 0.50 | 7.3/4.8 | |
22 | 0.05 | 4.9/3.7 |
| |||
R1 | TYK2 JH2 (IC50, μM) | IL23/IFNα (IC50, μM) | |
11 | 0.022 | 0.7/1.4 | |
18 | 0.007 | 0.1/0.05 | |
19 | 0.017 | 0.6/0.6 | |
20 | 0.11 | 6.2/4.1 | |
21 | 0.50 | 7.3/4.8 | |
22 | 0.05 | 4.9/3.7 |