Continued SAR exploration of 1,2,4-thiadiazole-containing scaffolds in the design of free fatty acid receptor 1 (GPR40) agonists

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      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.


      Original languageEnglish
      Number of pages10
      Pages (from-to)229-238
      JournalEuropean journal of medicinal chemistry
      Journal publication date13 Sep 2017
      Early online date13 Sep 2017
      StateEarly online date - 13 Sep 2017

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      • Journal Article

      ID: 136278469