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. 2019 Nov 27;9:17640. doi: 10.1038/s41598-019-54158-2

Table 1.

Structure-activity data of selected piperidine-pyridoindole analogs.

graphic file with name 41598_2019_54158_Figa_HTML.gif
Compound R1 R2 R3 EC50 (μM) Relative Vmax (%)*
A01 3-methoxy-benzyl H OMe 10 100
A061 2,4-difluoro-benzyl H OMe 2.0 100
A662 3,4-difluoro-benzyl H OMe 2.6 100
A666 graphic file with name 41598_2019_54158_Figb_HTML.gif H OMe 5.1 91
A357 benzyl H H 16 31
A534 3-methoxy-benzyl H H 13 24
A600 3-methoxy-benzyl Me H >30 4
A714 cyclohexyl H OMe >30 18
A815 graphic file with name 41598_2019_54158_Figc_HTML.gif H H >30 -4
A350 graphic file with name 41598_2019_54158_Figd_HTML.gif H OMe >30 7
A956 graphic file with name 41598_2019_54158_Fige_HTML.gif H OMe >30 6
A145 SO2-Me H OMe >30 7
A764 Me H OMe >30 6

*100% Vmax corresponds to 20 μM ASP-11.