Table 1.
GPR55 Antagonist Activity of Compounds.
| Entry, Compound | R | Ar | IC50a (95% CI) |
|---|---|---|---|
| 1,5at |
|
|
12 μM (3.9 - 36) |
| 2, 5au |
|
|
0.42 μM (0.075 - 2.4) |
| 3, 5av |
|
|
7.0 μM (0.47 - 100) |
| 4, 5aw |
|
|
insol.b |
| 5, 5bt |
|
|
insol.b |
| 6, 5bv |
|
|
insol.b |
| 7, 5bw |
|
|
1.8 μM (0.74 – 4.3) |
| 8, 5ct |
|
|
2.5 μM (1.3 – 5.0) |
| 9, 5dt |
|
|
0.64 μM (0.33 - 1.2) |
| 10, 5et |
|
|
0.77 μM (0.39 - 1.5) |
a
IC50 values and 95% confidence intervals (CI) were determined by running the sample in triplicate versus a 6 μM concentration of LPI
b
compound was not completely soluble at the concentrations of the assay.