Table 2.
Piperidine hit series 2 SAR determined in the human sperm calcium influx assay.[a]
|
| |||
|---|---|---|---|
|
Compd |
R1 |
R2 |
IC50 [μM] |
|
2 a |
|
Cl |
7.5±1.3 |
|
2 b |
|
H |
92±14 |
|
2 c |
|
Cl |
18±2 |
|
2 d |
|
18±7 |
|
|
2 e |
|
Cl |
>100 |
|
2 f |
|
Cl |
>100 |
|
2 g |
|
Cl |
>100 |
|
2 h |
|
Cl |
>100* |
|
2 i |
|
Cl |
>100* |
|
2 j |
|
Cl |
87* |
|
2 k |
|
>100* |
|
|
2 l |
|
>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.