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. 2016 Dec 15;8(4):700–712. doi: 10.1039/c6md00560h

Table 5. Improving PDE4 selectivity.

Inline graphic
R2 R3 TYK2 JH2 (IC50, μM) IL23/IFNα (IC50, μM) PDE4 (IC50, μM) LM % rem (h/r/m)
31 graphic file with name c6md00560h-u34.jpg graphic file with name c6md00560h-u35.jpg 0.013 0.51/0.41 2.4 41/4/3
32 graphic file with name c6md00560h-u36.jpg graphic file with name c6md00560h-u37.jpg 0.004 0.33/0.20 0.38 51/16/0
33 graphic file with name c6md00560h-u38.jpg graphic file with name c6md00560h-u39.jpg 0.066 1.2/1.1 >100 89/86/65
34 graphic file with name c6md00560h-u40.jpg graphic file with name c6md00560h-u41.jpg 0.025 0.41/0.32 >33 96/80/50
35 graphic file with name c6md00560h-u42.jpg graphic file with name c6md00560h-u43.jpg 0.008 0.78/0.75 5.6 75/75/34