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Dec. 10, 2021

Compound 44: a Bicyclic Macrocyclic Peptide PCSK9 Inhibitor

compound 44

bioavailable bicyclic macrocycle PCSK9 inh. %F cyno = 2.9, MW 1612, preclinical from mRNA display screen and SBDD Journal of Medicinal Chemistry Merck & Co.

Drug Hunter Team

The Merck bicyclic macrocyclic peptide PCSK9 inhibitor, “ compound 44 ,” is a highly potent (Ki = 0.00239 nM) and orally bioavailable (cyno %F = 2.9, t1/2 = 10 h) agent against a notoriously difficult target for small molecules, demonstrating target engagement comparable to approved PCSK9 antibodies. The discovery of this molecule is an [...]



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