Table 1.
Compound | KM (μM) | kcat (min-1) | kcat/KM (μM-1.min-1) | IC50(b) (μM) |
---|---|---|---|---|
1 | 0.39 ± 0.01 | 36 ± 2 | 90 | 0.7 ± 0.1 |
2 | n.d. | n.d. | n.d. | 0.7 ± 0.2 |
3 | 0.24 ± 0.07 | 5 ± 0.6 | 23 | 0.6 ± 0.1 |
4 | 0.14 ± 0.02 | 19 ± 1 | 141 | 0.4 ± 0.1 |
5 | 0.21 ± 0.02 | 23 ± 2 | 110 | 0.4 ± 0.2 |
6 | 0.32 ± 0.02 | 42 ± 5 | 132 | 0.7 ± 0.2 |
Kinetic constants were calculated for the formation of the major product upon oxidation of each compound by microsomes of insect cells expressing recombinant CYP2J2 (conditions described in Materials and Methods). Values are means ± SD from three independent experiments.
Values previously reported (33) for the inhibition of CYP2J2-catalyzed hydroxylation of ebastine by the indicated compound.
n.d.: not determined because of the formation of too low amounts of product.