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Updated: Apr 25, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Positive allosteric modulators for mGluR2 receptors: a medicinal chemistry perspective
György Szabó, György Miklós Keserű1
1Research Centre for Natural Sciences, Hungarian Academy of Sciences, P.O. Box 17, H-1525 Budapest, Hungary. gy.keseru@ttk.mta.hu.
Abstract:
This review summarizes drug discovery efforts on mGluR2 positive allosteric modulators (PAMs) from 2000 to 2013. Medicinal chemistry programs and the identified 21 chemotypes are analyzed and compared in terms of their biological activity and ligand efficiency. Comparative analysis of ligand efficiency metrics including ligand efficiency and lipophilic ligand efficiency allowed us to identify the most promising chemotypes. The perspective of their clinical development was evaluated in the light of recent human data.
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