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. Author manuscript; available in PMC: 2022 Jan 1.
Published in final edited form as: Vet Parasitol. 2020 Dec 15;289:109336. doi: 10.1016/j.vetpar.2020.109336

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)