Table 6.
Phthalazinone core hit series 6 SAR determined in the human sperm calcium influx assay.[a]
|
| |||
|---|---|---|---|
|
Compd |
R1 |
R2 |
IC50 [μM] |
|
6 a |
|
|
5.4±0.4 |
|
6 b |
|
|
8.3±1.1 |
|
6 c |
|
|
>100 |
|
6 d |
|
|
>100 |
|
6 e |
|
|
>100 |
[a] CatSper activated by 3 μM progesterone. IC50 values are means±SEM of three independent experiments.