(Q34135392)

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Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound

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31 July 2017

Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound (English)

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PubMed publication ID

31 July 2017

artificial neural network

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based on heuristic

inferred from title

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31 July 2017

Karen J. Gregory

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Karen J Gregory

13

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Colleen M. Niswender

14

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Colleen M Niswender

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31 July 2017

Craig W. Lindsley

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Craig W Lindsley

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31 July 2017

P. Jeffrey Conn

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P Jeffrey Conn

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31 July 2017

Christopher M. Olsen

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Christopher M Olsen

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31 July 2017

Alice L. Rodriguez

4

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Alice L Rodriguez

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31 July 2017

Brittney S Bates

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Brittney S Bates

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31 July 2017

Kyle A. Emmitte

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Kyle A Emmitte

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31 July 2017

2

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Eric S Dawson

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31 July 2017

Brian A Chauder

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Brian A Chauder

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31 July 2017

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Jeffrey P Lamb

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31 July 2017

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Danny G Winder

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31 July 2017

12

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Carrie K Jones

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31 July 2017

author name string

Ralf Mueller

1

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31 July 2017

Andrew S Felts

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31 July 2017

Usha N Menon

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31 July 2017

Sataywan B Jadhav

10

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31 July 2017

Alexander S Kane

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31 July 2017

publication date

20 January 2012

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31 July 2017

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31 July 2017

7

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31 July 2017

3

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31 July 2017

406-414

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31 July 2017

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

1 reference

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5 July 2018

(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction

1 reference

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5 July 2018

Recent advances in the design and development of novel negative allosteric modulators of mGlu(5)

1 reference

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5 July 2018

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

1 reference

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5 July 2018

Operant sensation seeking requires metabotropic glutamate receptor 5 (mGluR5).

1 reference

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5 July 2018

Operant sensation seeking in the mouse

1 reference

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5 July 2018

Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity

1 reference

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5 July 2018

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats

1 reference

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5 July 2018

Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening

1 reference

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5 July 2018

Metabotropic glutamate receptors: physiology, pharmacology, and disease

1 reference

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5 July 2018

Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.

1 reference

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5 July 2018

Recent progress in the discovery and development of negative allosteric modulators of mGluR5.

1 reference

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5 July 2018

Operant sensation seeking engages similar neural substrates to operant drug seeking in C57 mice

1 reference

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5 July 2018

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

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Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

1 reference

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5 July 2018

mGluR5 antagonists: discovery, characterization and drug development.

1 reference

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5 July 2018

Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

1 reference

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5 July 2018

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3517057

5 July 2018

A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3517057

5 July 2018

Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes

1 reference

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5 July 2018

Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity

1 reference

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5 July 2018

Metabotropic glutamate receptors as novel targets for anxiety and stress disorders

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The mGluR theory of fragile X mental retardation

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Neural networks as robust tools in drug lead discovery and development

1 reference

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5 July 2018

Targeting metabotropic glutamate receptors for treatment of the cognitive symptoms of schizophrenia

1 reference

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Direct and indirect modulation of the N-methyl D-aspartate receptor

1 reference

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5 July 2018

Modulation of the basal ganglia by metabotropic glutamate receptors: potential for novel therapeutics

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Hit and lead generation: beyond high-throughput screening

1 reference

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Glutamate receptors and Parkinson's disease: opportunities for intervention

1 reference

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5 July 2018

Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents

1 reference

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5 July 2018

Localization and physiological roles of metabotropic glutamate receptors in the direct and indirect pathways of the basal ganglia

1 reference

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Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice

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1 reference

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Heroin and cocaine intravenous self-administration in rats: Mediation by separate neural systems

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Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents.

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based on heuristic

inferred from PubMed ID database lookup

Virtual Screening for Selective Allosteric mGluR1 Antagonists and Structure–Activity Relationship Investigations for Coumarine Derivatives

1 reference

https://pubmed.ncbi.nlm.nih.gov/22267125

12 December 2020

based on heuristic

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1 reference

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7 January 2021

based on heuristic

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10.1002/CMDC.201100510

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Europe PubMed Central

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31 July 2017

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31 July 2017

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31 July 2017

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