Table 2:
Compound | R | PDE4D7- S129D IC50 (nM) |
PDE4B1- S133D IC50 (nM) |
PDE4D7- S129(wt) IC50 (nM) |
Ratio B/D |
Ratio Basal/Activated |
---|---|---|---|---|---|---|
12 | 4-CH2CH2OH | 9 | 562 | 2111 | 60 | 226 |
13 | 4-(CH2)2CONH2 | 35 | 166 | 1283 | 5 | 37 |
14 | 4-CH2CO-NMe2 | 51 | 356 | 914 | 7 | 18 |
15 | 4-CH2CO-N(H)Me | 133 | 98 | 1991 | 1 | 15 |
16 | 3- CH2CH2OH | 226 | 1419 | 6325 | 6 | 28 |
17 | 4-CH2CO2H | 1165 | 1642 | NTb | 1 | - |
See table 1 for assay definitions. See experimental section for methods and detailed synthetic procedures.
NT: Not tested