Properties of leading compounds^a.

Compd	HLM/RLM/MLM T1/2 (min)b	Human PPB (% bound)c	Mean Papp (10–6 cm s−1)		Efflux ratio
			A to B	B to A
1a	72/15.6/9.4	90.7	10.59	7.23	0.68
2d	29.7/9.4/6.9	92.5	9.46	5.04	0.53
2h	0.6/17.4/0.6	99.8	0.10	0.15	1.59
3b	10.1/27.5/28.9	>99	1.01	0.93	0.92
3c	7.7/15.4/19.0	>99	0.42	0.37	0.88
3n	7.5/8.9/16.7	99.4	5.14	4.55	0.89
3o	61.4/100.9/104.7	98.6	9.67	3.58	0.37
BTZ043	46.1/22.0/16.7	99.4	9.02	7.17	0.79
PBTZ169	11.1/14.7/14.4	99.6	0.74	0.74	1

^aPermeability was correlated with the apparent permeability coefficient P_app (cm s⁻¹), which was interpreted as follows: low permeability (P_app ≤ 1.0 × 10⁻⁶ cm s⁻¹), moderate permeability (1.0 × 10⁻⁶ < P_app < 5.5 × 10⁻⁶ cm s⁻¹) or high permeability (P_app ≥ 5.5 × 10⁻⁶ cm s⁻¹).

^bHLM = human liver microsomes, RLM = rat liver microsomes, MLM = mouse liver microsomes.

^cPPB = plasma protein binding.