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. 2022 Jun 14;17(15):e202000499. doi: 10.1002/cmdc.202000499

Table 2.

Piperidine hit series 2 SAR determined in the human sperm calcium influx assay.[a]

graphic file with name CMDC-17-0-g004.jpg

Compd

R1

R2

IC50 [μM]

2 a

graphic file with name CMDC-17-0-g064.jpg

Cl

7.5±1.3

2 b

graphic file with name CMDC-17-0-g068.jpg

H

92±14

2 c

graphic file with name CMDC-17-0-g029.jpg

Cl

18±2

2 d

graphic file with name CMDC-17-0-g024.jpg

18±7

2 e

graphic file with name CMDC-17-0-g014.jpg

Cl

>100

2 f

graphic file with name CMDC-17-0-g070.jpg

Cl

>100

2 g

graphic file with name CMDC-17-0-g007.jpg

Cl

>100

2 h

graphic file with name CMDC-17-0-g002.jpg

Cl

>100*

2 i

graphic file with name CMDC-17-0-g047.jpg

Cl

>100*

2 j

graphic file with name CMDC-17-0-g045.jpg

Cl

87*

2 k

graphic file with name CMDC-17-0-g025.jpg

>100*

2 l

graphic file with name CMDC-17-0-g027.jpg

>100*

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