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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 4.

Modification at N1 position of pyrazole core

graphic file with name nihms-1549696-t0032.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),
(%Emax)
AT1
Calcium
EC50*
(μM)
35. graphic file with name nihms-1549696-t0033.jpg 0.425 ± 0.06 (45) 0.344 ± 0.004 (91) 0.422 ± 0.008 (75) ND* ND
36. graphic file with name nihms-1549696-t0034.jpg 0.049 ± 0.004 (91) 0.107 ± 0.046 (110) 0.078 ± 0.02 (77) 0.060 ± 0.03 >10
25. graphic file with name nihms-1549696-t0035.jpg 0.081 ± 0.025 (91) 0.282 ± 0.08 (97) 0.144 ± 0.008 (90) 0.054 ± 0.01 >10
37. graphic file with name nihms-1549696-t0036.jpg 0.070 ± 0.009 (94) 0.097 ± 0.032 (106) 0.063 ± 0.004 (89) 0.059 ± 0.02 >10
38. graphic file with name nihms-1549696-t0037.jpg 0.101 ± 0.001 (87) 0.151 ± 0.04 (101) 0.092 ± 0.007 (78) 0.147 ± 0.06 >10
*

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

*

ND = Not Done