Table 3. In Vitro ADME of Selected Analogues.

entry	PAMPAa	Caco-2bA–B	Caco-2bB–A	CYP Met CL-Msc(ER)	CYP Met CL-rat(ER)	CYP Met CL-Hud(ER)	hERGe IC50(μM)
15	52	0.70	2.55	0.47	nt	<0.21	nt
22	51.8	1.26	2.99	0.48	0.66	0.49	13.4
24	51.5	0.61	1.3	0.46	0.69	0.53	>30
27	81	3.05	8.38	0.51	0.63	0.52	5.6
28	99.5	1.2	0.97	0.4	0.89	0.55	21.9
29	99.5	3.5	2.37	0.41	0.79	0.47	>30
31	99.5	8.2	2.36	0.87	0.96	0.79	nt
32	80.9	15	14.37	0.66	0.95	0.44	nt
33	nt	nt	nt	0.72	nt	nt	nt
34	97.1	3.22	3.35	0.61	0.68	0.72	>30
35	99.9	15.56	6.96	0.87	0.93	0.88	nt
36	99.9	nt	nt	0.8	0.92	0.92	nt

^aMeasured as percentage absorbed.

^bunits = (cm/s ×10⁶).

^cMs = mouse.

^dHu = human.

^eQ-patch assay; nt = not tested.