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ID: ALA4190352
Journal: Eur J Med Chem
Title: Continued SAR exploration of 1,2,4-thiadiazole-containing scaffolds in the design of free fatty acid receptor 1 (GPR40) agonists.
Authors: Krasavin M, Lukin A, Bakholdina A, Zhurilo N, Onopchenko O, Borysko P, Zozulya S, Moore D, Tikhonova IG.
Abstract: An earlier reported series of 1,2,4-thiadiazole-based agonists of FFA1 (GPR40) was evolved into two structurally distinct series of compounds. One of the series (structurally related to known FFA1 agonist GW9508) displayed low micromolar potency while the other (representing a truncated version of the earlier reported potent FFA1 agonists) was, surprisingly, found to be devoid of agonist potency. In silico docking of representative compounds into the crystal structure of FFA1 revealed possible structural grounds for the observed SAR.
CiteXplore: 28938138