Table 5.
Scaffold 4
| # | -R1 | -R2 | -R3 | IC50 (95% CI),μM | Hill slope (95% CI) |
|---|---|---|---|---|---|
| 4aa | -H | -CH3 |
|
inactivea | |
| 4ab | -H |
|
|
weak inhibitora | |
| 4ac | -H |
|
|
297 (180 – 490) | −1.3 (−2.3, −0.4) |
| 4ad | -H |
|
|
weak inhibitora | |
| 4ae | -H |
|
|
inactive | |
| 4af | -H |
|
|
weak inhibitora | |
| 4ag | -H |
|
|
inactive | |
| 4ah | -H |
|
|
inactivea | |
| 4ai | -H |
|
|
inactivea | |
| 4aj | -H |
|
|
weak inhibitora | |
| 4ak | -H |
|
|
inactivea | |
| 4al | -H |
|
|
inactivea | |
| 4am | -H |
|
|
stimulator | |
| 4an | -H |
|
|
inactive | |
| 4ao | -H |
|
|
17 (9–31) | −1.1 (−1.6, −0.5) |
| 4ap |
|
|
-H | inactivea | |
| 4aq |
|
|
-H | inactivea | |
| 4ar |
|
|
-H | weak inhibitora | |
| 4as |
|
|
-H | inactive | |
| 4at |
|
|
-H | 28 (20 – 40) | −1.2 (−1.5, −0.8) |
| 4au |
|
|
-H | stimulatora | |
| 4av |
|
|
-H | inactivea | |
| 4aw |
|
|
-H | inactive | |
| 4ax |
|
|
-H | 89 (52–153) | −1.2 (−1.8, −0.5) |
a
modulatory effect estimated from three concentrations only;
b
4-parameter logistic model curve could not be fitted