. Author manuscript; available in PMC: 2014 Oct 10.

Published in final edited form as: J Med Chem. 2013 Sep 30;56(19):10.1021/jm401067s. doi: 10.1021/jm401067s

Table 3.

Biochemical and cell-based activities, microsome stability and CYP inhibition properties of inhibitors 14.^a

		K_D (nM)	EC₅₀ (µM)	Microsome stability t_1/2 (min)			%inhibition of human CYPs (at 1 µM, unless indicated otherwise)
	R			h	Rat	m	1A2	2C9	2D6	3A4
3r		<5	0.16	6	3	3	51^b	96^b	84^b	86^b
14a		<5	0.39	4	9	4	18^b	95^b	88^b	90^b
14b		<5	0.11	12	6	3	19^b	98^b	90^b	98^b
14c		<5	0.25	8	9	5	48^b	99^b	97^b	98^b
14d		<5	0.88	5	7	5	78^b	99^b	98^b	91^b
14e		<5	0.66	7	4	4	58^b	99^b	95^b	91^b
14f		38	0.35	8	8	6	46^b	99^b	92^b	92^b
14g		80	0.59	6	11	4	28^b	96^b	95^b	97^b
14h		95	0.21	6	9	3	29	86	64	80
14i		<5	0.33	25	6	4	32	89	59	94
14j		60	0.036	9	8	4	42	94	86	90
14k		30	0.13	12	4	4	34	93	76	94
14l		<5	0.26	11	9	8	76^b	99^b	96^b	95^b
14m		<5	0.54	18	7	6	47	97	88	91
14n		<5	0.33	14	9	8	18	94	86	65
14o		50	0.46	29	23	18	41	95	73	77
14p		<5	0.55	19	19	23	67^b	99^b	95^b	92^b
14q		<5	0.89	10	6	5	80^b	99^b	98^b	92^b
14r		50	0.37	16	15	25	36	87	61	56
14s		<5	0.30	16	20	24	32	82	58	68
14t		<5	0.19	17	25	36	31	85	54	73

See notes to Table 1

CYP inhibition for this compound was performed at 10 µM