. Author manuscript; available in PMC: 2014 Oct 24.

Published in final edited form as: J Med Chem. 2013 Oct 10;56(20):10.1021/jm401266k. doi: 10.1021/jm401266k

Table 3.

Inhibition of CYP3A4.

Cmpd	IC₅₀^a	% TDI^b	k_obs^c	k_obs ratio^d
4	0.34	66	0.0921	6.01
5	> 50	4	0.0023	0.11
8	> 50	3	0.0003	0.01
10	1.1	< 1	0.0028	0.15
11	0.04	36	0.0386	1.78

inhibition of midazolam turnover, μM

normalized percent activity remaining (12 min preincubation with cmpd at 10 μM)

inactivation rate, min⁻¹

ratio of inactivation rates between compound and ethynylestradiol (< 1 considered low TDI potential).