molecules of the month


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

Structure of SCO-267, a full agonist of the GPCR GPR40
1 min read

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, clogP = 5.8). The compound is orally active in a rodent obesity model and was advanced to a Ph. I study.

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