. Author manuscript; available in PMC: 2017 Mar 15.

Published in final edited form as: Bioorg Med Chem. 2016 Feb 3;24(6):1314–1321. doi: 10.1016/j.bmc.2016.02.002

Table 2.

Caco-2 permeability coefficients (P_app) of drug 2 and selected prodrugs, and relative amount of prodrug remaining intact at 2 h in apical side (RA_AP) and in basolateral side (RA_BL). AP-BL and BL-AP signs signify the donor solution is in apical and basolateral side, respectively.

Compound	P_app (×10⁻⁶ cm/s)		Efflux ratio	RA_AP (%)		RA_BL (%)

	AP-BL^a	BL-AP^a		AP-BL	BL-AP	AP-BL	BL-AP
2¹⁶	4.2	1.3	0.3
3	1.1	1.6	1.5	93	88	81	86
5	0.5	3.5	7.0	74	15	63	93
7	3.9	6.9	1.8	29	1	3	90
9	0.4	3.4	8.5	88	53	73	95
10	0.5	3.8	7.6	97	78	90	99

donor concentration = 100 µM