Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 6, Pages 2841-2846Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01962
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Funding
- Danish Council for Independent Research, Technology and Production [09-070364]
- Danish Council for Strategic Research [11-116196]
- University of Southern Denmark [SDU2020]
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The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.
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