Table 1:
Properties of BKI-1369
Compound | C. parvum CDPK1 IC50 (μM) | Human SRC IC50 (μM) | NIuc-C. parvum EC50 (μM) | Mammalian cytotox CC50 (μM) | Cardiotox hERG IC50 (μM) | MUTAGEN/GENOTOX | Aqueous SOLUBILITY (μM) | % PLASMA PROTEIN BINDING | |
---|---|---|---|---|---|---|---|---|---|
BKI-1369 | 0.0009 | >10 | 2.5 | >80 | 1.5 | (−) | 100 | 77 | 40 |
Human | Dog | ||||||||
>80 | 54 | 40 | 76 | ||||||
Mouse | Rat |
IC50: Concentration in micromolar (μM) that gives 50% inhibition of enzyme activity; Human SRC: Proto-oncogene tyrosine-protein kinase SRC; CC50: concentration that yields 50% growth inhibition (cytotoxicity) of mammalian CRL-8155 or HEPG2 cell lines; hERG: human ether-a-go-go related gene, a potassium channel found in heart tissue; Modified AMES test is the AMES test that includes liver microsome metabolized compound; Aqueous endpoint solubility performed at 2 pHs shown; and plasma protein binding shows the bound percentage of compound when incubated with plasma from species shown. Adapted from data in (Hulverson et al., 2017a; Hulverson et al., 2017b)