Table 3. CYP and hERG Inhibition of Coumarin.
CYP inhibition
IC50 (μM)a |
|||
---|---|---|---|
compd | 2C9 (−/+) | 3A4 (−/+) | hERG inhibitonb (%) |
11a | 29/96 | 13/5.6 | ND |
11d | >100/>100 | >100/>100 | ND |
14 | 19/19 | 26/11 | 25 |
1 | 12/60 | >100/>100 | no inhibition |
IC50 (−) and IC50 (+) values were determined after a 30 min preincubation without and with NADPH, respectively.
At 10 μM.