Delving into the Latest Updates on VU-6031545 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

mGluR5

Action

negative allosteric modulator

Mechanism

mGluR5 negative allosteric modulator(Metabotropic glutamate receptor 5 negative allosteric modulator)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Pain

Inactive Indication-

Originator Organization

Vanderbilt University

Active Organization

Vanderbilt University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: Peng, Weimin ; Felts, Andrew S. ; Cho, Hyekyung P. ; Temple, Kayla J. ; Lindsley, Craig W. ; Bender, Aaron M. ; Engers, Julie L. ; Crocker, Katherine E. ; Chang, Sichen ; Capstick, Rory A. ; Niswender, Colleen M. ; Henderson, Scott H. ; Billard, Natasha B. ; Blobaum, Anna L. ; Han, Changho ; Rodriguez, Alice L. ; Maurer, Mallory A. ; O’Neill, Jordan ; Whomble, David L. ; Conn, P. Jeffrey ; Rook, Jerri M. ; Watson, Katherine J. ; Boutaud, Olivier

This Letter describes the discovery of novel mGlu₅ NAMs VU6031545 and VU6024945. Starting from previously reported picolinamide compounds, a structure-activity relationship study of various core isosteres was conducted, leading to the identification of thieno[3,2-b]pyridine-5-carboxamide and 2,3-difluorobenzamide as competent core replacements. These compounds are highly potent as well as brain penetrant with an IVIVC agreement and improved oral bioavailability in rats.

100 Deals associated with VU-6031545

Login to view more data