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. 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.[a]

graphic file with name CMDC-17-0-g052.jpg

Compd

R1

R2

IC50 [μM]

6 a

graphic file with name CMDC-17-0-g039.jpg

graphic file with name CMDC-17-0-g061.jpg

5.4±0.4

6 b

graphic file with name CMDC-17-0-g072.jpg

graphic file with name CMDC-17-0-g010.jpg

8.3±1.1

6 c

graphic file with name CMDC-17-0-g077.jpg

graphic file with name CMDC-17-0-g055.jpg

>100

6 d

graphic file with name CMDC-17-0-g038.jpg

graphic file with name CMDC-17-0-g017.jpg

>100

6 e

graphic file with name CMDC-17-0-g035.jpg

graphic file with name CMDC-17-0-g073.jpg

>100

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