Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM) (original) (raw)

Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)

Scott Throner

Bioorganic & Medicinal Chemistry Letters, 2011

Discovery of 1‑Butyl-3-chloro-4-(4-phenyl-1-piperidinyl)- (1H)‑pyridone (JNJ-40411813): A Novel Positive Allosteric Modulator of the Metabotropic Glutamate 2 Receptor

Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2

Alexandro Donizeti Nunes

Journal of Medicinal Chemistry, 2017

3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization

Ivan Efremov

Bioorganic & Medicinal Chemistry Letters, 2009

Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N -(4-(2-Methoxyphenoxy)phenyl)- N -(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine

James Monn

Journal of Medicinal Chemistry, 2003

Discovery of 1,4-Disubstituted 3-Cyano-2-pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

Corey Hopkins

Bioorganic & Medicinal Chemistry Letters, 2009

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators

Huiyong Yin

Bioorganic & Medicinal Chemistry Letters, 2008

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

uyen le

Bioorganic & Medicinal Chemistry Letters, 2009

Scaffold Hopping From Pyridones to Imidazo [1, 2-a] Pyridines. New Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptor

Gregor MacDonald

Bioorganic & medicinal …, 2010

LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors

Paul Ornstein

Neuropharmacology, 1998

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Corey Hopkins

Bioorganic & Medicinal Chemistry Letters, 2010

New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): Identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones

Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites

Jean-philippe Pin

Journal of medicinal chemistry, 2018

Discovery of 1,5-Disubstituted Pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

Discovery of 2-(2-Benzoxazoyl amino)-4-Aryl-5-Cyanopyrimidine as Negative Allosteric Modulators (NAMs) of Metabotropic Glutamate Receptor 5 (mGlu 5 ): From an Artificial Neural Network Virtual Screen to an In Vivo Tool Compound

ChemMedChem, 2012

CTEP: A Novel, Potent, Long-Acting, and Orally Bioavailable Metabotropic Glutamate Receptor 5 Inhibitor

Neil Parrott

Journal of Pharmacology and Experimental Therapeutics, 2011

Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators

Valerie Whiterock

ACS Medicinal Chemistry Letters, 2016

Structures of mGluRs shed light on the challenges of drug development of allosteric modulators

John Christopher, Fiona Marshall

Current opinion in pharmacology, 2015

4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators

Megan Nattini

Bioorganic & Medicinal Chemistry Letters, 2012

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4)

Bioorganic & medicinal chemistry letters, 2016

1,3,5-Trisubstituted Pyrazoles as Potent Negative Allosteric Modulators of the mGlu2/3 Receptors

Fabrice Jourdan

ChemMedChem, 2017

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Journal of Medicinal Chemistry, 2015

Structure−Activity Relationships Comparing N-(6-Methylpyridin-yl)-Substituted Aryl Amides to 2-Methyl-6-(substituted-arylethynyl)pyridines or 2-Methyl-4-(substituted-arylethynyl)thiazoles as Novel Metabotropic Glutamate Receptor Subtype 5 Antagonists

Journal of Medicinal Chemistry, 2009

Pharmacological Characterization of a New, Orally Active and Potent Allosteric Metabotropic Glutamate Receptor 1 Antagonist, 4-[1-(2-Fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC)

奈穂子金子

Journal of Pharmacology and Experimental Therapeutics, 2007

Reprint of Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2

Thomas Woltering

Neuropharmacology, 2017

Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5

Bioorganic & Medicinal Chemistry Letters, 2011

Exploring the Active Conformation of Cyclohexane Carboxylate Positive Allosteric Modulators of the Type 4 Metabotropic Glutamate Receptor

Jean-philippe Pin

ChemMedChem, 2014