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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