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. 2020 Nov 16;10:19889. doi: 10.1038/s41598-020-77056-4

Table 4.

Summary of in vitro ADME for compound 10.

Compounds CYP1A2 CYP2C9 CYP2C19 CYP2D6 CYP3A4
CYP isozyme activity (% of control activity)
Compound 10 36.7 97.4 12.1 95.1  > 100
Ketoconazole (reference) 99.1 97.5 > 100 99.0 25.0
Ketoconazole: CYP3A4 inhibitor (0.1 µM)
Compounds Human (%) Rat (%)
Human and rat liver microsomal stability (% remaining during 30 min)
Compound 10 9.5 5.2
Verapamil (reference) 15.3
Compounds Human Rat
30 min 120 min 30 min 120 min
Human and rat plasma stability (% remaining)
Compound 10 98.1 91.6 93.8 87.5
Procaine (reference) 1.5 (5 min) 0.4 (10 min) 89.8 52.6
Enalapril (reference) 95.0 93.7 37.7 1.8