molecules of the month

Compound 33

intravenous PKG1α activator

satisfactory in vivo rat PK profile

from 2.9 M compounds HTS, SBDD and opt

J. Med. Chem.

Merck & Co., Inc., South San Francisco, CA

Compound 33 Chemical Structure intravenous PKG1α activator - Merck & Co., Inc., South San Francisco, CA
5 mins read

Context. “Compound 33” (Merck) is a cGMP-dependent protein kinase G1α (PKG1α) activator cGMP modulation is considered one of the most promising approaches for cardiovascular drug discovery with >30 agents either approved for use or in various stages of clinical development. Although PKGs are the main effector of cGMP, cardiovascular drug discovery efforts focusing on this target have not yielded similar success as those observed for guanylate cyclases and phosphodiesterases (PDEs). This is likely attributable to the complexity of the PKG architecture and an incomplete understanding of the mechanisms underlying PKG activation. Current preclinical agents are either cGMP analogs or synthetic peptides. The tool “compound 33” was developed based on the hypothesis that allosteric activation of PKG by a small molecule…

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