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. Author manuscript; available in PMC: 2022 May 14.
Published in final edited form as: ACS Infect Dis. 2021 Feb 10;7(5):1200–1207. doi: 10.1021/acsinfecdis.0c00803

Table 1.

In vitro properties of pyrrolopyrimidines, BKI-1812, BKI-1814, and BKI-1649.

BKI-1812 BKI-1814 BKI-1649
CpCDPK1
IC50 (μM) 		0.0025 0.005 0.0022
C. parvum
EC50 (μM) 		0.52 1.39 1.03
CRL-8155
CC50 (μM) 		>80 >80 >40
HepG2
CC50 (μM) 		>80 >80 >40
Solubility
pH 2.0 (μM) 		>100 >100 >100
Solubility
pH 6.5 (μM) 		96.5 >100 83
hERG
IC50 (μM) 		>44 >39 >30
Modified Ames Negative Negative ND*
In vitro mononucleus genotoxicity Negative Negative ND*
Plasma Protein Binding Mouse 85.0% 99.9% 94%
Plasma Protein Binding Rat 91.5% 94.7% 90%
Plasma Protein Binding Human 99.9% 99.9% 56%

ND = not done