SCO-267 is a full agonist of the GPCR GPR40, whose activation stimulates secretions of insulin and incretin. Since no crystal structures were available, the authors used conformational modeling to rationally improve the ligand from a weak lipophilic initial starting point (0.4 uM, clogP 9.4) to a more lipophilically efficient candidate (12 nM [...]
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Sep. 18, 2021
SCO-267: An Oral Full Agonist of GPR40
SCO-267
oral full agonist of GPR40 GCPR oral efficacy in obesity model, entered Ph. I from optimization of prior molecule J. Med. Chem., Sep. 24, 2020 Takeda / SCOHIA Pharma, Fujisawa, JP