Table 5. In Vitro ADME of Selected Analogues^a.

				hepatic microsome metabolic stability (extraction ratio)
compd	PAMPA (% absorbed)	Caco-2 A–B (cm/s × 106)	Caco-2 B–A (cm/s × 106)	mouse	rat	human	hERG (Q-patch) IC50 (μM)
5	52	0.70	2.55	0.47	nt	<0.21	nt
11	81	3.05	8.38	0.51	0.63	0.52	5.6
18	low	0.56	2.32	0.31	nt	nt	>30
24	92	1.07	2.6	0.46	nt	nt	5.7
25	52	1.63	3.58	0.17	nt	nt	11.1
26	96	0.96	1.66	0.19	0.87	0.54	1.5
27	52	0.44	1.25	0.17	0.63	0.55	nt
28	89	1.46	1.86	0.17	0.43	0.54	2.3
29	low	0.99	2.99	0.21	0.38	0.21	nt
30	86	0.14	1.03	0.17	0.12	0.39	4.8
31	low	0.75	0.96	0.57	0.6	0.37	21
32	94	0.84	0.87	0.76	0.67	0.48	5.6

^ant = not tested.