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. 2022 Apr;381(1):42–53. doi: 10.1124/jpet.121.001075

Table 1.

Effective doses of cGMP-PDE inhibitors

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.