Table 2.
Scaffold 1
| -R1 | -R2 | -R3 | IC50 (95% CI),μM | Hill slope (95% CI) | |
|---|---|---|---|---|---|
| 1aa | -H | 2-CH3; 3-Cl | -OH | 18 (15 – 22) | −2.3 (−4.2, −0.5) |
| 1ab | -H |
|
-OH | 63 (44 – 91) | −1.3 (−1.7, −0.7) |
| 1ac | -Cl | 2-Cl; 5-Cl | -OH | 13 (9 – 17) | −1.3 (−1.7, −0.8) |
| 1ad | -CH3 | -H |
|
weak inhibitora | |
| 1ae | -CH3 | -H |
|
118 (76 – 184) | −0.9 (−1.2, −0.5) |
| 1af | -CF3 | -H |
|
76 (42 – 137) | −1.2 (−1.9, −0.4) |
| 1ag | -CF3 | -H |
|
170 (115 – 250) | −1.7 (−2.5, −09) |
| 1ah | -CF3 | -H |
|
140 (87 – 225) | −1.3 (−1.9, −0.6) |
| 1ai | -CF3 | -H |
|
143 (74 – 276) | −0.8 (−1.3, −0.3) |
| 1aj | -OCF3 | -H |
|
49 (37 – 66) | −2.2 (−3.2, −1.2) |
| 1ak | -OCF3 | -H |
|
98 (75 – 128) | −1.9 (−3.1, −0.8) |
a
modulatory effect estimated from three concentrations only.