. 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 4.

Biochemical and cell-based activities, microsome stability and CYP inhibition properties of inhibitors 27.^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
14t		<5	0.19	17	25	36	31	85	54	73
27a		<5	0.57	19	12	20	14	87	68	41
27b		<5	0.28	18	13	23	14	85	58	63
27c		<5	1.0	18	41	50	0	71	20	43
27d		<5	0.28	12	15	22	3	77	34	58
27e		<5	0.97	35	22	27	0	75	37	14
27f		<5	0.98	21	36	53	10	80	34	41
27g		<5	0.28	16	10	19	33	92	70	74
27h		<5	0.97	22	20	32	48	93	75	54
27i		<5	0.014	23	32	14	10	91	38	69
27j		<5	0.22	6	14	22	15	87	32	57
27k		<5	0.23	34	125	83	0	85	16	21
27l		<5	0.25	31	32	29	11	94	68	92
27m		<5	0.20	20	19	17	29	91	57	90
27n		<5	0.98	>120	67	104	23 (26)^b	88 (96)^b	28 (68)^b	28 (46)^b
27o		<5	0.98	70	67	53	21 (25)^b	90 (94)^b	63 (85)^b	25 (33)^b
27p		<5	0.47	28	31	25	12	94	83	79
27q		<5	0.057	13	19	7	10 (44)^b	74 (98)^b	66 (89)^b	54 (94)^b
27r		<5	0.018	7	19	3	37	97	85	61
27s		<5	0.46	15	36	41	5 (21)^b	16 (71)^b	22 (81)^b	39 (82)^b
27t		-	0.039	4	26	20	0	87	51	61

See notes to Table 1

Values in parentheses are % inhibition of the indicated human CYPs at 10 µM