Table 3.
Inhibition of PDE9 and its mutants by inhibitors 1r and 1s
Proteins | IC50 (nM) 1s | IC50 (nM) 1r |
---|---|---|
wildtype | 88±17 | 22±3 |
L420A | 607±31 | 179±17 |
Y424A | 471±19 | 190±10 |
F456A | 159±9×103 | 14±2×103 |
Q453A | 50±5×103 | 9.6±1.3×103 |
M365A | 103±6 | 46±4 |
F441A | 129±9 | 43 ± 1 |
I403A | 519±26 | 200±25 |