Table 2.

Biochemical and cell-based activities, microsome stability and CYP inhibition properties of inhibitors 3.^a

				KD (nM)	EC50 (µM)	Microsome stability t1/2 (min)			%inhibition of human CYPs (at 10 µM)
	R1	R2	R3			h	rat	m	1A2	2C9	2D6	3A4
3a				n/bb	n/ec	5	2	2	25	16	30	50
3b				n/b	n/e	4	4	2	24	39	5	22
3c				n/b	n/e	>120	59	47	0	25	37	25
3d				n/b	n/e	97	53	51	2	25	63	19
3e				n/b	n/e	45	32	11	6	61	65	54
3f				n/b	n/e	16	39	7	−26	13	69	23
3g				<5	-	-	-	-	-	-	-	-
3h				91	-	-	-	-	-	-	-	-
3i				<5	3.0	3	3	2	22	96	91	96
3j				220	n/e	86	26	21	12	98	89	94
3k				<5	0.58	4	3	2	76	99	98	99
3l				792	3.2	6	7	5	14	98	86	94
3m				<5	0.90	5	3	2	26	99	93	98
3n				<5	0.61	6	3	2	44	98	91	99
3o				<5	0.30	4	3	3	64	99	96	97
3p				12	1.6	4	4	2	33	99	91	99
3q				14	0.85	3	3	3	54	99	96	99
3r				<5	0.16	6	3	3	51	96	84	86

^aSee notes to Table 1

^bn/b: no binding at 10 µM

^cn/e: not effective at 10 µM