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. 2019 Jan 24;8(1):114–125. doi: 10.1002/open.201800282

Table 1.

Analogues of C38 with substituents on the central phenyl ring, synthesized via Scheme 1.

graphic file with name OPEN-8-114-g008.jpg
Cmpd Structure K i hAT2R [nM][a] [%] Inhibition of hAT1R at 10 μM[b]
C38 graphic file with name OPEN-8-114-g009.jpg 270 (19[c]) IC50=694 nM[d] 7 IC50>10 000 nM[e]
40 graphic file with name OPEN-8-114-g010.jpg 300 IC50=217 nM[d] 8 IC50>10 000 nM[e]
41 graphic file with name OPEN-8-114-g011.jpg 120 13
42 graphic file with name OPEN-8-114-g012.jpg 800 16
43 graphic file with name OPEN-8-114-g013.jpg 230 14
44 graphic file with name OPEN-8-114-g014.jpg 810 26
45 graphic file with name OPEN-8-114-g015.jpg 800 12
46 graphic file with name OPEN-8-114-g016.jpg 120 18
47 graphic file with name OPEN-8-114-g017.jpg 280 1.8
48 graphic file with name OPEN-8-114-g018.jpg 1300 23
49 graphic file with name OPEN-8-114-g019.jpg 660 19
50 graphic file with name OPEN-8-114-g020.jpg 230 22
51 graphic file with name OPEN-8-114-g021.jpg 310 9.7

[a] Radioligand displacement from hAT2R in membranes from HEK‐293 cells overexpressing hAT2R (assay 1). N=6 for C38 and 40, N=2 for all other. [b] Inhibition of radioligand binding from hAT1R expressed in HEK‐293 cells (assay 1). [c] Radioligand displacement from AT2R in pig uterus membrane.29 [d] Radioligand displacement from hAT2R expressed in HEK‐293 cells (assay 2). [e] Radioligand displacement from hAT1R expressed in HEK‐293 cells, ligands were not active on hAT1R at the concentrations tested (assay 2). N=9.