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. 2015 Nov;43(11):1670–1678. doi: 10.1124/dmd.115.065987

TABLE 2.

Comparison of IC50 values of known inhibitors obtained using the single-substrate approach, the new cocktail approach, and literature values

Substrate Inhibitor Single Substrate IC50 ± S.D. Cocktail IC50 ± S.D. Literature IC50
µM µM µM
CYP1A2 Phenacetin Furafylline 3.70 ± 1.00 3.58 ± 0.49 0.48–13.88 (Eagling et al., 1998; Testino and Patonay, 2003; Walsky and Obach, 2004; Zientek et al., 2008; Otten et al., 2011; Kozakai et al., 2012; Liu et al., 2015)
CYP2A6 Coumarin Methoxsalen 0.40 ± 0.03 0.48 ± 0.05 0.21–2.11 (Kim et al., 2005; Workman and Raynaud, 2007; Kozakai et al., 2012)
CYP2B6 Bupropion Ticlopidine 0.70 ± 0.08 1.06 ± 0.10 0.1–0.78 (Turpeinen et al., 2005; Otten et al., 2011)
CYP2C8 Amodiaquine Quercetin 5.92 ± 0.54 3.40 ± 0.32 1.09–7.00 (Dierks et al., 2001; Walsky and Obach, 2004; Otten et al., 2011; Liu et al., 2015)
CYP2C9 Tolbutamide Sulfaphenazole 0.53 ± 0.06 0.90 ± 0.10 0.069–1.30 (Eagling et al., 1998; Shader et al., 1999; Testino and Patonay, 2003; Workman and Raynaud, 2007; Zientek et al., 2008; Otten et al., 2011; Kozakai et al., 2012; Yao et al., 2012; Qin et al., 2014; Liu et al., 2015)
CYP2C19 (S)-mephenytoin Ticlopidine 3.40 ± 0.32 5.81 ± 0.80 0.86–4.46 (Giancarlo et al., 2001; Zientek et al., 2008; Yao et al., 2012; Qin et al., 2014; Liu et al., 2015)
CYP2D6 Dextromethorphan Quinidine 0.46 ± 0.02 0.84 ± 0.10 0.009–0.52 (Shader et al., 1999; Testino and Patonay, 2003; Walsky and Obach, 2004; Zientek et al., 2008; Otten et al., 2011; Kozakai et al., 2012; Yao et al., 2012; Qiao et al., 2014; Qin et al., 2014; Liu et al., 2015)
CYP3A4/5 Midazolam Ketoconazole 0.094 ± 0.006 0.115 ± 0.056 0.01–0.13 (Patki et al., 2003; Walsky and Obach, 2004; Workman and Raynaud, 2007; Otten et al., 2011; Kozakai et al., 2012; Yao et al., 2012; Qiao et al., 2014; Qin et al., 2014; Liu et al., 2015)
Testosterone 0.062 ± 0.004 0.054 ± 0.002 0.008–0.0477 (Eagling et al., 1998; Patki et al., 2003; Walsky and Obach, 2004; Kozakai et al., 2012; Yao et al., 2012; Qiao et al., 2014)
CYP2E1 Chlorzoxazone Diethyldithiocarbamate 12.42 ± 1.70 22.58 ± 5.60 9.8–16.6 (Eagling et al., 1998; Shader et al., 1999; Workman and Raynaud, 2007)