Table 7.
Triazolopyridazine hit series 7 SAR determined in the human sperm calcium influx assay.[a]
|
| |||
|---|---|---|---|
|
Compd |
R1 |
R2 |
IC50 [μM] |
|
7 a |
m‐Me |
|
20±1 |
|
7 b |
m‐Me |
|
>100 |
|
7 c |
m‐Me |
|
58±5 |
|
7 d |
p‐Me |
|
25±3 |
|
7 e |
p‐Me |
|
21.7±0.4 |
|
7 f |
p‐Me |
|
68±6 |
|
7 g |
m‐Me |
|
35±10 |
[a] CatSper activated by 3 μM progesterone. IC50 values are means±SEM of three independent experiments.