TABLE 2

Comparison of literature values for KI and kinact with values estimated from data generated using the automated time-dependent inhibition assay described in this article




CYP

KI

kinactmin-1

Literature KI

Literature kinact

Referencesa
μM min-1 μM min-1
Troleandomycin 3A4 0.26 0.121 0.18-0.73 0.15-0.27 1, 2, 3
Mifepristone 3A4 0.61 0.080 0.5-4.7 0.089-0.18 3, 4
Erythromycin 3A4 8.82 0.120 5-82 0.011-0.173 2, 5, 6, 7, 8, 9
Diltiazem 3A4 0.49 0.010 2 0.015-0.17 1, 3, 8, 10
Verapamil 3A4 0.74 0.041 1.7-5.9 0.09-1.1 1, 3, 11
Ethinylestradiol 3A4 23 0.09 18 0.04 12
Tienilic acid 2C9 0.85 0.23 4.3 0.2 14
MDMA 2D6 6.4 0.23 13 0.29 13
Ticlopidine
2C19
9.2
0.25
87
0.19
14