Table 5. Improving PDE4 selectivity.
| ||||||
R2 | R3 | TYK2 JH2 (IC50, μM) | IL23/IFNα (IC50, μM) | PDE4 (IC50, μM) | LM % rem (h/r/m) | |
31 | 0.013 | 0.51/0.41 | 2.4 | 41/4/3 | ||
32 | 0.004 | 0.33/0.20 | 0.38 | 51/16/0 | ||
33 | 0.066 | 1.2/1.1 | >100 | 89/86/65 | ||
34 | 0.025 | 0.41/0.32 | >33 | 96/80/50 | ||
35 | 0.008 | 0.78/0.75 | 5.6 | 75/75/34 |