Table 4.

ADMET Properties of Compound 26

Assay	Compound 26
liver microsomes (human or mouse, 0.1 μM)	103.3% or 90.1%
cryopreserved hepatocytes (human, 1 μM)	85.7%
CYP inhibition (10 μM)
CYP1A	17%
CYP2C9	30%
CYP2C19	21%
CYP2D6	44%
CYP3A	10%
hERG inbihition (0.1, 1, 10 μM)	4%, 7%, 23%
plasma protein binding (human or mouse, 10 μM)	31% or 11%
A-B permeability (Caco-2, pH 7.4/7.4)	90.9 × 10−6 cm/s
A-B permeability (Caco-2, pH 7.4/7.4 + verapamil)	79.2 × 10−6 cm/s
B-A permeability (Caco-2, pH 7.4/7.4)	18.4 × 10−6 cm/s
B-A permeability (Caco-2, pH 7.4/7.4 + verapamil)	55.2 × 10−6 cm/s
Ames test (strain TA98, TA100, TA1535, TA1537, with/without S9)	Negative