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. Author manuscript; available in PMC: 2022 Oct 14.
Published in final edited form as: ChemMedChem. 2022 Jun 14;17(15):e202000499. doi: 10.1002/cmdc.202000499

Table 6.

Phthalazinone core hit series 6 SAR determined in the human sperm calcium influx assay

graphic file with name nihms-1812278-t0049.jpg
Compound R1 R2 IC50, μM
6a graphic file with name nihms-1812278-t0050.jpg graphic file with name nihms-1812278-t0051.jpg 5.4 ± 0.4
6b graphic file with name nihms-1812278-t0052.jpg graphic file with name nihms-1812278-t0053.jpg 8.3 ± 1.1
6c graphic file with name nihms-1812278-t0054.jpg graphic file with name nihms-1812278-t0055.jpg > 100
6d graphic file with name nihms-1812278-t0056.jpg graphic file with name nihms-1812278-t0057.jpg > 100
6e graphic file with name nihms-1812278-t0058.jpg graphic file with name nihms-1812278-t0059.jpg > 100

CatSper activated by 3 μM progesterone. IC50 values are means ± SEM of 3 independent experiments.