. Author manuscript; available in PMC: 2011 May 13.

Published in final edited form as: J Med Chem. 2010 May 13;53(9):3685–3695. doi: 10.1021/jm100057h

Table 4.

Inhibition of cytochrome P450 isoforms by the test articles at 1 and 10 μM. Data expressed as percent metabolism of known substrates for each isoform compared to control.^a

Name	CYP Inhibition (metabolite produced as a percent of control)
	CYP2B6		CYP2C9		CYP2C19		CYP2D6		CYP3A4^a		CYP3A4^b
	1 μM	10 μM	1 μM	10 μM	1 μM	10 μM	1 μM	10 μM	1 μM	10 μM	1 μM	10 μM
CQ	112	134	114	128	113	111	99	90	105	110	102	106
1	119	118	118	115	120	126	101	72	114	125	102	125
2	99	109	105	145	109	115	81	57	107	120	108	120
3	97	121	103	126	93	107	94	94	94	111	96	113
4	95	112	102	121	107	115	83	63	101	108	103	105
5	108	107	109	73	104	114	61	13	89	30	76	26
6	98	117	98	96	104	120	55	22	103	92	102	82
7	111	108	113	104	97	108	60	15	101	94	99	89
8	114	115	119	122	117	136	23	8	109	96	107	84
9	104	117	107	108	108	110	85	49	108	85	102	89
10	96	113	97	106	103	119	56	15	103	85	94	57
11	98	114	96	79	108	107	98	10	97	63	80	39
12	96	100	98	79	90	102	61	13	90	69	87	75
13	108	128	107	128	110	113	94	87	105	102	102	88
14	98	113	93	63	107	115	64	17	101	68	92	53
15	106	109	104	100	104	127	73	20	100	82	99	87
16	94	107	85	46	101	106	53	11	97	57	89	46
17	99	110	102	93	94	123	79	4	89	66	84	62
18	94	112	98	115	104	121	76	29	99	66	96	70
19	103	98	102	102	100	119	91	56	101	102	103	90
20	105	105	108	108	113	122	96	69	106	108	108	97

The known substrates are as follows: CYP2B6 (bupropion 25 μM), CYP2C9 (diclofenac 10 μM), CYP2C19 (mephenytoin 50 μM), CYP2D6 (bufuralol 10 μM), CYP3A4a (midazolam 4μM), and CYP3A4b (testosterone 50 μM). Values <70% are considered to be significant inhibition.