Table 3. Activity of Selected Compounds in Functional Cellular Assays in Agonist.
| entry | compd | GTPγS agonist modea (Emax at 20 μM) | GTPγS antagonist modeb (IC50/inhibition at 2 μM) |
|---|---|---|---|
| 1 | 25 | –11% | 64 nM/107% |
| 2 | 28 | –10% | 10 nM/110% |
| 3 | 43 | –15% | 2.8 nM/102% |
| 4 | 48 | –8% | 37 nM/105% |
| 5 | 53 | –10% | 20 nM/112% |
| 6 | 55 | –17% | 85 nM/106% |
| 7 | 60 | no effectc | 46 nM/85% |
| 8 | 61 | +7% | 57 nM/80% |
| 9 | 63 | –10% | 3.7 nM/94% |
a
In the absence of PGD2, 100% represents the level of stimulation given by 2 μM PGD2.
b
In the presence of 80 nM PGD2.
c
No statistically significant effect (−5% < effect < 5%).