Delving into the Latest Updates on GT-949 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

EAAT2

Mechanism

EAAT2 modulators(solute carrier family 1 member 2 modulators)

Therapeutic Areas

Nervous System Diseases

Active Indication

Central Nervous System Diseases

Inactive Indication-

Originator Organization

The Wistar Institute

Active Organization

Drexel University College of Medicine

Inactive Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC30H37N7O2

InChIKeyZVWPOIUAPXDLMB-UHFFFAOYSA-N

CAS Registry460330-27-2

Excitatory amino acid transporters (EAATs) are essential CNS proteins that regulate glutamate levels. Excess glutamate release and alteration in EAAT expression are associated with several CNS disorders. Previously, we identified positive allosteric modulators (PAM) of EAAT2, the main CNS transporter, and have demonstrated their neuroprotective properties in vitro. Herein, we report on the structure-activity relationships (SAR) for the analogs identified from virtual screening and from our medicinal chemistry campaign. This work identified several selective EAAT2 positive allosteric modulators (PAMs) such as compounds 4 (DA-023) and 40 (NA-014) from a library of analogs inspired by GT949, an early generation compound. This series also provides nonselective EAAT PAMs, EAAT inhibitors, and inactive compounds that may be useful for elucidating the mechanism of EAAT allosteric modulation.

100 Deals associated with GT-949

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