Table 3.
Modification of carboxylic acid moiety of 26.
 |
| Compd. | R | n | APJ Calcium EC50* μM±SEM (%Emax) |
APJ cAMP EC50* μM±SEM (%Emax) |
APJ β-arrestin EC50* μM±SEM (%Emax) |
APJ Binding Ki* (μM±SEM) (%Emax) |
AT1 Calcium EC50* (μM±SEM) |
|---|---|---|---|---|---|---|---|
| 26. | -OH | 0 | >10 | >10 | >10 | ND* | ND |
| 27. |  |
0 | 0.021± 0.007 (131) | 3.09 ± 3.0 (124) | 2.33 ± 0.9 (119) | 0.187± 0.06 | ND |
| 28. |  |
0 | 0.027 ± 0.02 (106) | 0.266 ± 0.057 (106) | 0.207 ± 0.002 (99) | 0.134± 0.09 | >10 |
| 29. |  |
0 | 0.411± 0.09 (97) | >10 | >10 | ND | ND |
| 30. |  |
0 | 0.313± 0.01 (93) | >10 | >10 | ND | ND |
| 31. |  |
0 | 0.162± 0.001 (98) | >10 | 8.67± 0.1 (54) | 0.571± 0.3 | >10 |
| 32. |  |
0 | 1.26 ± 0.8 (81) | 3.48± 0.1 (13) | >10 | ND | ND |
| 33. | -OH | 1 | >10 | >10 | >10 | ND | ND |
| 34. |  |
1 | 0.083± 0.01 (96) | >10 | 3.11 ± 0.2 (80) | 0.449± 0.08 | >10 |
*
EC50 and Ki values are averages of multiple experiments performed in duplicate ± standard error of the mean.
*
ND = Not Done