TABLE 3

Lysosomal trapping of reference compounds in rat hepatocytes

Data are expressed as mean ± S.E.M. of duplicate measurements from hepatocytes of three individual rats. Physicochemical data (log D7.5, basic pKa values) were calculated by ADMET Predictor.

CompoundLog DpH 7.5Highest Basic pKaSecond Highest Basic pKaLysosomal Trapping IC50Cytotoxicity IC50
µMµM
Chloroquine2.49.97.33.9 ± 0.5>100
Diclofenac2.4>100>100
Fluoxetine3.29.88.0 ± 2.4>100
Imipramine2.192.24.8 ± 1.2>100
Olaparib1.60.2>100>100
Propranolol1.89.415 ± 2.1>100