Delving into the Latest Updates on VU-6036864 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

M5 receptor

Action

antagonists

Mechanism

M5 receptor antagonists(Muscarinic acetylcholine receptor M5 antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication

Nervous System Diseases

Inactive Indication-

Originator Organization

Vanderbilt University

Active Organization

Vanderbilt University

Inactive Organization-

License Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC15H16ClN5O3S

InChIKeyURAUBDCJGRESTK-CQOLUAMGSA-N

CAS Registry2746406-36-8

Author: Maurer, Mallory A. ; Nader, Michael A. ; Jackson, Megan ; Chang, Sichen ; Vinson, Paige N. ; Rodriguez, Alice L. ; Engers, Julie L. ; Han, Changho ; Lindsley, Craig W. ; Blobaum, Anna L. ; Orsi, Douglas L. ; Presley, Christopher C. ; Han, Allie ; Bubser, Michael ; Long, Madeline F. ; Boutaud, Olivier ; Li, Jinming ; Capstick, Rory A. ; Conn, P. Jeffrey ; Niswender, Colleen M. ; Cho, Hyekyung P. ; Jones, Carrie K.

While the muscarinic acetylcholine receptor mAChR subtype 5 (M₅) has been studied over decades, recent findings suggest that more in-depth research is required to elucidate a thorough understanding of its physiological function related to neurological and psychiatric disorders. Our efforts to identify potent, selective, and pharmaceutically favorable next-generation M₅ antagonist tool compounds have led to the discovery of a novel triazolopyridine-based series. In particular, VU6036864 (45) showed exquisite potency (human M₅ IC₅₀ = 20 nM), good subtype selectivity (>500 fold selectivity against human M_1-4), desirable brain exposure (K_p = 0.68, K_p,uu = 0.65), and high oral bioavailability (%F > 100%). VU6036864 (45) and its close analogues will support further studies of M₅ as advanced antagonist tool compounds and play an important role in the emerging biology of M₅.

100 Deals associated with VU-6036864

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