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. 2014 Nov 25;57(23):10192–10197. doi: 10.1021/jm501375c

Table 1. Structure and Activities of Analogues 9.

graphic file with name jm-2014-01375c_0008.jpg

entry R GLP-1R EC50 (μM) GLP-1R pEC50a GLP-1R maxa (%)
(S)-8 Et 2.4 5.69 ± 0.12 53.4 ± 2.03
(S)-9a n-Pr 6.5 5.18 ± 0.13 48.4 ± 2.77
(S)-9b i-Pr 1.3 5.88 ± 0.15 59.2 ± 2.53
(S)-9c 2-OMeBn 12.1 4.92 ± 0.09 68.3 ± 3.31
(S)-9d n-hexyl 10.3 4.99 ± 0.09 55.7 ± 2.63
(S)-9e CH2CH2Ph 14.1 4.74 ± 0.19 68.5 ± 7.96
a

GLP-1 pEC50 and GLP-1 max data reported as averages + SEM from our calcium mobilization assay; n = 3.