. Author manuscript; available in PMC: 2019 Dec 13.

Published in final edited form as: J Med Chem. 2018 Nov 30;61(23):10910–10921. doi: 10.1021/acs.jmedchem.8b01671

Table 1. Microsomal stability: half-lives and estimated clearance of the compounds in human, rat, and mouse liver microsomes.

(R² values were all >0.7)

Compound	Human			Rat			Mouse
Compound	Cl_int^a	Cl_hep	t_½ (min)^b	Cl_int	Cl_hep	t_½ (min)	Cl_int	Cl_hep	t_½ (min)
VFV	29.9	12.3	42	17.7	14.2	158	145	55.6	38
VFV-Cl	13.9	8.35	90	35.5	23.6	79	59.8	35.9	91
2	22.3	10.8	56	29.7	20.8	95	105	48.4	52
3	23.5	11.1	53	52.3	29.9	54	99.0	47.1	55
4	20.9	10.5	60	142	46.9	20	34.2	24.8	160
5	21.2	10.6	58	131	45.6	22	220	63.9	25
6	11.6	7.46	108	58.1	31.7	48	127	52.6	43
7	19.4	10.1	64	55.8	31.1	50	237	65.2	23
8	16.5	9.24	76	64.3	33.5	48	87.7	44.4	62
9	7.53	5.54	166	30.9	21.4	91	55.8	34.5	98

Estimated intrinsic (Cl_int) and hepatic clearance (Cl_hep) expressed in mL/min/kg body weight,

in vitro half-life values in minutes.