Table 1.
Pharmacological potency of PF-04418948 in relevant recombinant systems
| Antagonist activity | Agonist activity | ||
|---|---|---|---|
| Functional reporter assay | KB (nM) | IC50 (nM) | EC50 (nM) |
| Human EP2 | 1.8 (95% CI 0.3–9.3, n = 4) | 16 (95% CI 11.7–21.8, n = 22) | >33 300 (n = 2) |
| Human EP1 | >10 000 (n = 1) | >10 000 (n = 1) | |
| Human EP3 | >10 000 (n = 1) | >10 000 (n = 1) | |
| Human EP4 | >33 300 (n = 2) | >33 300 (n = 2) | |
| Human DP1 | >32 800 (n = 8) | ND | |
| Human CRTH2 | 32 000 (n = 2) | ND |
| Binding | Ki (nM) | ||
|---|---|---|---|
| Human IP | >10 000 (n = 2) | ||
| Human FP | >10 000 (n = 2) | ||
| Human TP | >10 000 (n = 2) | ||
| Human LTB4 | 4800 (n = 1) |
ND, not determined.