|
Lipophilicity |
s1 Receptor Binding Parameters |
Compound |
k´w |
ClogP |
IC50 (nM) |
Ki (nM) |
Hill Slope |
|
|
|
|
|
|
4, 2-F; n = 4 |
ND |
5.03 |
17.48 ± 0.31 |
12.08 ± 0.22 |
-1.07 ± 0.01 |
|
|
|
|
|
|
5, 3-F; n = 4 |
ND |
5.03 |
11.21 ± 1.29 |
7.74 ± 0.89 |
-1.13 ± 0.09 |
|
|
|
|
|
|
6, 4-F; n = 4 |
2.54 ± 0.05 |
5.03 |
11.34 ± 2.02 |
7.83 ± 1.39 |
-1.21 ± 0.05 |
|
|
|
|
|
|
7, 2-Br; n = 3 |
3.09 ± 0.05 |
5.75 |
26.62 ± 3.95 |
18.39 ± 2.73 |
-0.78 ± 0.03 |
|
|
|
|
|
|
8, 3-Br; n = 3 |
3.06 ± 0.07 |
5.75 |
9.14 ± 0.85 |
6.35 ± 0.59 |
-1.02 ± 0.15 |
|
|
|
|
|
|
9, 4-Br; n = 3 |
3.31 ± 0.08 |
5.75 |
9.85 ± 3.92 |
6.80 ± 2.71 |
-1.00 ± 0.02 |
|
|
|
|
|
|
10, 2-I; n = 2 |
ND |
6.01 |
62.47 ± 0.96 |
43.15 ± 0.66 |
-1.12 ± 0.03 |
|
|
|
|
|
|
11, 4-I; n = 4 |
3.71 ± 0.05 |
6.01 |
22.89 ± 0.94 |
15.82 ± 0.65 |
-1.59 ± 0.08* |
|
|
|
|
|
|
|