2. Academic Validation
  3. MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate

MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate

  • ACS Med Chem Lett. 2018 Apr 30;9(7):652-656. doi: 10.1021/acsmedchemlett.8b00095.
Douglas C Beshore 1,  Christina N Di Marco 1,  Ronald K Chang 1,  Thomas J Greshock 1,  Lei Ma 1,  Marion Wittmann 1,  Matthew A Seager 1,  Kenneth A Koeplinger 1,  Charles D Thompson 1,  Joy Fuerst 1,  George D Hartman 1,  Mark T Bilodeau 1,  William J Ray 1,  Scott D Kuduk 1
Affiliations

Affiliation

  • 1 MRL, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.
PMID: 30034595 DOI: 10.1021/acsmedchemlett.8b00095
Abstract

Identification of ligands that selectively activate the M1 muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physicochemical and safety properties, ultimately leading to the clinical candidate MK-7622, a highly selective positive allosteric modulator of the M1 muscarinic receptor that has entered Phase II studies in patients with Alzheimer's disease.

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