TABLE 1

Ki values (μM) obtained with five probe substrates, i.e., (S)-flurbiprofen, (S)-warfarin, phenytoin, tolbutamide, and diclofenac, using CYP2C9.1

Global standard error for data fitting was less than 15% and r2 > 0.9 for each effector.

Inhibitors
Flurbiprofen
Warfarin
Phenytoin
Tolbutamide
Diclofenac
Mibefradil 11.10 1.04 6.75 6.63 13.79
Indomethacin 53.41 0.66 15.76 14.24 14.47
Benzbromarone 0.004 0.001 0.04 0.02 0.01
Sulfaphenazole 0.06 0.12 0.23 0.22 0.15
Nicardipine 0.07 0.01 0.33 0.03 0.03
(S)-Ibuprofen 4.27 3.06 4.02 3.95 4.46
Amiodarone 2.10 2.99 4.03 0.69 1.89
Sulfamethizole 17.90 2.22 13.08 7.17 14.69
Omeprazole 5.33 0.64 2.16 0.92 0.41
Clozapine 4.13 3.46 12.88 11.00 11.43
Gemfibrozil 12.43 0.79 2.38 2.83 3.64
Ketoconazole 0.38 0.08 1.81 1.79 1.52
Progesterone 1.72 1.41 4.30 4.01 5.20
Nifedipine 1.14 0.34 1.35 0.84 0.57
Thiobendazole >100 17.22 36.21 33.09 41.08
Quinine 3.45 19.80 85.53 76.35 >100
Quercetin 1.18 0.25 0.27 0.14 0.13
Fluvoxamine 0.63 0.58 2.46 2.74 4.12
Tamoxifen 3.44 0.66 3.77 3.32 4.67
Miconazole 0.03 0.01 0.11 0.05 0.04
α-Naphthoflavone 0.78 0.29 0.75 0.34 0.41
Diclofenac 1.60 1.24 1.64 0.75
Flurbiprofen 3.27 16.38 19.86 11.35
Warfarin 4.17 4.35 2.13 3.52
Phenytoin 5.58 4.04 6.65 9.02
Tolbutamide 1.54 1.00 4.70 3.41
Piroxicam 0.47 0.92 18.27 15.18 4.02
Vivid Green 8.21 0.53 1.72 1.05 0.84
Dapsone
Activator
0.09
7.10
9.49
5.29