Table 1.
Target | Drug | IC50 | EC50a | Human Plasma [Cmax] |
---|---|---|---|---|
PDE5 | Sildenafil | 3.9 nM(Gupta et al., 2005) | 66-271 µM (Li et al., 2013; Mei et al., 2015) | 1.2 µM(Gupta et al., 2005) (100 mg dose) |
Tadalafil | 1-5 nM(Gupta et al., 2005; Ahmed, 2018) | 38 µM(Li et al., 2013) | 0.87 µM(Gupta et al., 2005) (20 mg dose) | |
Exisulind | 113 µM(Soh et al., 2000) | 165-557 µM(Thompson et al., 2000) | 13-27 µM(van Stolk et al., 2000) (40-200 mg dose) | |
PDE9 | Pf-04447943 | 12 nM(Charnigo et al., 2019) | 90 µMb | 0.12-0.63 µM (Charnigo et al., 2019) |
BI-409306 | 52 nM(Rosenbrock et al., 2019) | ND | 1.37 µM(Moschetti et al., 2016) (100 mg dose) | |
PDE10 | TAK-063 | 0.3 nM(Harada et al., 2015) | 22 µMb | 0.57 µM(Tsai et al., 2016) (1000 mg dose) |
Pf-2545920 | 0.16 nM(Lee et al., 2016) | 14-20 µM(Lee et al., 2016) | 0.1-0.52 µM(Delnomdedieu et al., 2017) (10-30 mg dose) |
aInhibition of colon cancer cell growth.
bFrom the present study. ND: Not determined.