Table 1. Lead Series of SSTR5 Antagonists.

^aAll IC₅₀ values calculated are the mean of at least duplicate experiments within a maximal 3-fold range. N.D. = not determined.

^bPotency against human (h) and mouse (m) SSTR5.

^chERG inhibition measured by competitive binding with MK-499, a known hERG blocker.

^dDecrease in oral glucose AUC vs vehicle in male C57BL/6 mice fed with HFD (D12492) for 21 days, n = 3, t = 0–120 min, compound dosed 1 h before glucose.