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Sep. 17, 2021

Compound 9: M3-Selective Positive Allosteric Modulator

“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

Drug Hunter Team

“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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