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. 2018 Oct 5;9(11):1088–1093. doi: 10.1021/acsmedchemlett.8b00306

Table 2. Representative Analogues from the Chromane and Indole Subclasses of Spiropiperidine SSTR5 Antagonists.

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a

IC50 values were calculated as the mean of minimally duplicate experiments with less than threefold variance for acceptance of results.

b

Binding inhibition at 10 μM compound concentration.

c

Inhibition of forskolin-induced cAMP in CHO cells expressing human (h) or mouse (m) SSTR5.

d

Maximal inhibition at 8.3 mM compound concentration.

e

Percent parent compound after incubation at 1 μM for 30 min in 250 mg of protein/mL of microsomes from human (H) or rhesus monkey (Rh). N.D. = not determined.