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. 2015 Jul 20;6(9):1015–1018. doi: 10.1021/acsmedchemlett.5b00247

Table 1. Effect of Linker on Human GPR139 Potency.

graphic file with name ml-2015-00247a_0005.jpg

Cmpd linker EC50 (nM)a Emax (%)b
7h Gly 33 ± 7 146
10 l-Ala 66 ± 17 143
11 d-Ala 440 ± 34 88
12 l-Ser 283 ± 46 107
13 l-Phe 10 000 ND
a

Data are reported as mean ± SEM from at least three experiments.

b

The efficacy of l-Trp was set to 100%.