Table 1.
No. | R1 | R2 | Ar | Ke (OX1, nM)b | Ke (OX2, nM)c | OX2/OX1 | clogP |
---|---|---|---|---|---|---|---|
6 | Pr | Ph | 16.1 ± 3.6 | >10,000 | >621 | 6.86 | |
12a | Pr | Ph | 121 ± 35 | a | >82.6 | 7.29 | |
12b | Pr | Ph | 28.8 ± 4.4 | a | >347 | 6.98 | |
12c | Pr | Ph | 141 ± 42 | a | >70.9 | 7.40 | |
12d | Pr | Ph | 173 ± 5 | >10,000 | >58 | 6.17 | |
12f | Pr | Ph | 20.6 ± 2.8 | a | >485 | 6.17 | |
12g | Pr | Ph | 96.4 ± 34 | >10,000 | >104 | 5.96 | |
15a | CF3CH2 | 3-Py | 29.5 ± 2.2 | 1750 ± 230 | 59 | 5.70 | |
15b | CF3CH2 | 3-Py | 20.4 ± 2.9 | 1360 ± 150 | 67 | 5.39 | |
19a | CF3CH2 | Ph | 884 ± 70d | a | >11 | 4.47 | |
19b | CF3CH2 | Ph | >10,000d | a | 0 | 4.47 | |
19c | CF3CH2 | Ph | 1,860 ± 140d | a | >5.4 | 4.47 | |
25a | MeSO2 | Ph | 43.0 ± 18 | a | >232 | 5.25 | |
25b | MeSO2 | Ph | 5.24 ± 1.0 | 1,200 ± 360 | 229 | 5.19 |
< 50% inhibition at 10 μM final concentration;
Values are the mean of at least three independent experiments in duplicate;
Values are the mean of at least two independent experiments in duplicate; for compounds with Ke < 100 nM at OX1 at least three independent experiments in duplicate were performed.
Compound appeared insurmountable during standard assay procedure, so incubation was increased to 1 hour.