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. Author manuscript; available in PMC: 2017 Jul 14.
Published in final edited form as: J Med Chem. 2016 Jul 1;59(13):6531–6546. doi: 10.1021/acs.jmedchem.6b00760

Table 1.

Enzymatic TgCDPK1 and Src inhibition (IC50), hERG inhibition (IC50), HepG2 and CRL-8155 growth inhibition (GI50) and T. gondii cellular assay (EC50) results for compounds with variable R2 substructures (19). IC50 and GI50 values are the averages of at least three assays. T. gondii cellular assay EC50 values are the average of at least two runs that were performed in triplicate.

graphic file with name nihms825821u2.jpg
R2 IC50 (μM)
human cells, GI50 (μM)
EC50 (μM)
TgCDPK1 Src hERG HepG2 CRL-8155 T. gondii
1 graphic file with name nihms825821t1.jpg 0.0029 >10 0.40 >10 >10 0.14
5 graphic file with name nihms825821t2.jpg 0.0032 >10 1.7 >10 >10 0.283
6 graphic file with name nihms825821t3.jpg 0.0060 >10 1.4 >10 >10 0.41
7 graphic file with name nihms825821t4.jpg 0.010 >10 0.30 >10 >10 0.51
8 graphic file with name nihms825821t5.jpg 0.011 >10 >10 >10 >10 0.22
9 graphic file with name nihms825821t6.jpg 0.004 1.1 >10 >10 >10 0.48