molecules of the month

“Compound 9”

M3-selective positive allosteric modulator

oral bioavailability in rodent

from HTS and optimization

Bioorg. Med. Chem. Apr. 23, 2020

Astellas Pharma, Tsukuba, JP

Compound 9
1 min read

“Compound 9” is the first potent M3-selective positive allosteric modulator, with potential utility as a biological tool compound. It does have secondary activity against M5 at high doses though. It’s quite a large zwitterion, which is somewhat unusual for GPCRs.

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