Table 1.
Enzyme | Substrate | Model | IC50 (μmol/L) | Ki (μmol/L) | Reference |
---|---|---|---|---|---|
CYP3A4 | Testosterone | Human liver microsome | 4.0 | Piver et al. 2001 | |
Rat liver microsome | 20 | Piver et al. 2001 | |||
Recombinant isozyme | 10 | Piver et al. 2001 | |||
Recombinant isozyme | 15 | Piver et al. 2003 | |||
Human liver microsome | 25 | Piver et al. 2003 | |||
Recombinant isozyme | 1.1 | Yu et al. 2003; | |||
CYP3A11 (homolog) | Aripiprazole Nifedipine | Recombinant isozyme Mouse liver microsome |
6.8 15.8 |
Zhan et al. 2015Wang et al. 2015 | |
CYP1A1 | EROD | Human HepG2 microsome | 1.0 | 0.42 | Ciolino and Yeh 1999 |
Human HepG2 cell | 1.0 | Ciolino and Yeh 1999 | |||
Human MCF‐7 cell | 0.5 | Ciolino and Yeh 1999 | |||
Recombinant isozyme | 1.2 | Chang et al. 2001 | |||
Recombinant isozyme | 40 | Piver et al. 2001 | |||
Recombinant isozyme | 30 | Piver et al. 2003; | |||
CYP1A2 | EROD | Recombinant isozyme | 15.5 | Chang et al. 2001 | |
Recombinant isozyme | 30 | Piver et al. 2001 | |||
Human liver microsome | 25 | Piver et al. 2003 | |||
Phenacetin | Mouse liver microsome | 127.3 | Wang et al. 2015 | ||
CYP1B1 | EROD | Recombinant isozyme | 0.8 | Chang et al. 2001 | |
Recombinant isozyme | 40 | Piver et al. 2003 | |||
CYP2B1 | EFC | Rat liver microsomea | Huynh and Teel 2002 | ||
CYP2B6 | BROD | Recombinant isozyme | >50 | Piver et al. 2003 | |
Recombinant isozyme | 100 | Piver et al. 2003 | |||
Human liver microsome | 100 | Piver et al. 2003 | |||
CYP2D6 | Bufuralol | Human liver microsome | > 50 | Yu et al. 2003 | |
Aripiprazole | Recombinant isozyme | 87.9 | Zhan et al. 2015 | ||
CYP2E1 | Chlorzoxazone | Human liver microsome | 150 | Piver et al. 2001 | |
Recombinant isozyme | 50 | Piver et al. 2003; | |||
Human liver microsome Mouse liver microsome | 74.3 | 50 | Piver et al. 2003Wang et al. 2015 | ||
PNPH | Rat liver microsome | 18.5 | Mikstacka et al. 2002 | ||
CYP2C9 | Diclofenac | Human liver microsome | >50 | Yu et al. 2003 | |
CYP 2C19 | DBF | Human liver microsome | 22.5 | Orsini et al. 2016 |
BROD, 7‐benzoxy resorufin; EFC, 7‐ethoxy‐4‐trifluormethyl courmarin; EROD, 7‐ethoxyresorufin; DBF, O‐benzylfluorescein benzyl ester; PNPH, p‐nitrophenol hydroxylase.
P < 0.05 for percent inhibition.