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. Author manuscript; available in PMC: 2021 Feb 15.
Published in final edited form as: Bioorg Med Chem. 2019 Nov 30;28(4):115237. doi: 10.1016/j.bmc.2019.115237

Table 2.

Modification of carboxylic acid moiety of 12

graphic file with name nihms-1549696-t0015.jpg
Compd. R APJ
Calcium EC50*
μM±SEM
(%Emax)		 APJ
cAMP
EC50*
μM±SEM
(%Emax)		 APJ
β-arrestin
EC50*
μM±SEM
(%Emax)		 APJ
Binding
Ki*
(μM±SEM)		 AT1
Calcium
EC50*
(μM±SEM)
17. -NH2 5.75 ± 1.1 (94) >10 7.24 ± 0.9 (133) ND* ND
18. graphic file with name nihms-1549696-t0016.jpg 0.288 ± 0.03 (92) 0.684 ± 0.1 (105) 0.280 ± 0.001 (89) ND ND
19. graphic file with name nihms-1549696-t0017.jpg 0.237 ± 0.04 (91) 1.85 ± 0.2 (106) 0.453 ± 0.014 (87) ND ND
20. graphic file with name nihms-1549696-t0018.jpg 1.85 ± 0.5 (77) 4.82 ± 1.1 (129) 8.87 ± 2.7 (87) ND ND
21. graphic file with name nihms-1549696-t0019.jpg 0.046 ± 0.008 (88) 0.118 ± 0.02 (104) 0.113 ± 0.02 (89) 0.036 ± 0.006 >10
22. graphic file with name nihms-1549696-t0020.jpg 0.069 ± 0.02 (139) 0.157 ± 0.08 (104) 0.114 ± 0.005 (90) 0.038 ± 0.01 >10
23. graphic file with name nihms-1549696-t0021.jpg 0.144 ± 0.03 (102) 0.246 ± 0.02 (106) 0.182 ± 0.045 (87) 0.172 ± 0.1 >10
24. graphic file with name nihms-1549696-t0022.jpg 1.70 ± 0.04 (94) 3.17 ± 0.8 (134) 0.313 ± 0.04 (81) ND ND
25. graphic file with name nihms-1549696-t0023.jpg 0.081 ± 0.02 (91) 0.283 ± 0.08 (97) 0.144 ± 0.008 (90) 0.054 ± 0.01 >10
*

EC50 and Ki values are averages of multiple experiments performed in duplicate unless otherwise stated ± standard error of the mean.

*

ND = Not Done