molecules of the month

“compound 12j”

potent ghrelin receptor full agonist

for atrophy/cachexia, not advanced due to PK

from HTS and ligand-based design

J. Med. Chem., Aug. 12, 2020

Astrazeneca, Molndal, SE

Structure of compound 12j
1 min read

“compound 12j” is a potent agonist of the ghrelin hormone receptor, activation of which stimulates growth hormone secretion and appetite among other activities. Ghrelin receptor antagonists have previously been explored to treat disorders related to obesity such as diabetes, but an agonist could be useful in treating atrophic disorders like cachexia. Compound 12j has improved off-target selectivity versus a previously reported compound and has significant bioavailability in dogs, but was not advanced due to uncertainty about projected human oral exposure.

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