Table 1.
Summary of in vitro activities
| Assay | Compound‐1 | Compound‐2 | Compound‐3 | CJ‐023,423 | CJ‐042,794 |
|---|---|---|---|---|---|
| cAMP Antagonism (hEP4) | IC50 (nmol/L) ± SEM | IC50 (nmol/L) ± SEM | IC50 (nmol/L) ± SEM | IC50 (nmol/L) ± SEM | IC50 (nmol/L) ± SEM |
| Human EP4 | 5.6 ± 1.1; n = 8 | 5.6 ± 1.0; n = 10 | 2.4 ± 1.4; n =5 | 11.7 ± 3.0; n = 6 | 4.5 ± 1.85; n = 153 |
| Rat EP4 | 12.3, n = 1 | 15.4; n = 1 | 1.0, n = 1 | 13.1 ± 1.0; n = 5 | 20.6 ± 1.8; n = 20 |
| hEP1‐4 receptor binding | Ki (nmol/L) ± SEM | ||||
| EP1 | >17500; n = 2 | >17500; n = 3 | >17500; n = 1 | >22900; n = 1 | >26700; n = 2 |
| EP2 | >18900; n = 4 | 1210 ± 509; n = 6 | >18900; n = 1 | >21600; n = 2 | 931 ± 457; n = 6 |
| EP3 | >14000; n = 4 | >14000; n = 5 | >14000; n = 1 | >19500; n = 1 | >15500; n = 1 |
| EP4 | 58 ± 12; n = 10 | 41 ± 7; n = 12 | 2.07 ± 1.31; n = 8 | 449 ± 123; n = 8 | 12.6 ± 7.36; n = 6 |
| Human whole blood | IC50 (nmol/L) ± SD | IC50 (nmol/L) ± SD | IC50 (nmol/L) ± SD | IC50 (nmol/L) ± SD | IC50 (nmol/L) ± SD |
| (Reversal of PGE2 Inhibited TNFα) | 123 ± 80; n =8 | 123 ± 88; n =12 | 42 ± 17; n = 9 | 1560 ± 105; n = 79 | 840 ± 630; n = 15 |
Data are expressed as geometric mean ± standard deviation or standard error as noted.