253 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Gedeon Richter
Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu
Institute For Advanced Chemistry of Catalonia (Iqac-Csic)
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.
Eli Lilly
Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Bristol-Myers Squibb
Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.
Eli Lilly
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Merck Research Laboratories
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.
Bristol-Myers Squibb Research & Development
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.
Vanderbilt University Medical Center
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III.
University of Copenhagen
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Merck Research Laboratories
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5.
Shenyang Pharmaceutical University
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.
Vanderbilt University Medical Center
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.
Gedeon Richter
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Janssen Pharmaceutica
Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.
University of Copenhagen
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.
Vanderbilt University Medical Center
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.
Vanderbilt University Medical Center
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective
Eli Lilly
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.
Massachusetts General Hospital
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
Heptares Therapeutics
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.
Vanderbilt University Medical Center
Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators.
Toray Industries
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.
University of Modena and Reggio Emilia
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
Vanderbilt University Medical Center
Discovery and biological evaluation of tetrahydrothieno[2,3-c]pyridine derivatives as selective metabotropic glutamate receptor 1 antagonists for the potential treatment of neuropathic pain.
Korea Institute of Science and Technology
Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.
University of Maryland
Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Roche Pharmaceutical Research and Early Development
Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5.
University of Maryland
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization.
Gedeon Richter
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Janssen Pharmaceutica
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization.
Gedeon Richter
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Vanderbilt University Medical Center
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.
Vanderbilt University Medical Center
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Vanderbilt University Medical Center
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Pfizer
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).
National Institute of Mental Health
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
Merz Pharmaceuticals
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Vanderbilt University Medical Center
Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).
Vanderbilt University
Trisubstituted imidazoles as positive modulators of metabotropic glutamate receptor subtype 5.
Dart Neuroscience
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.
Janssen Pharmaceutica
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.
Vanderbilt University Medical Center
Discovery, synthesis, and structure-activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators.
Merz Pharmaceuticals
Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators.
Lundbeck Research Usa
Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
Sk Biopharmaceuticals
Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator.
Eli Lilly
Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.
Lundbeck Research Usa
Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain.
Brain Science Institute
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.
TBA
3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators.
Vanderbilt University
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.
Gedeon Richter
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
Glaxosmithkline
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.
Glaxosmithkline
Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold.
Vanderbilt University Medical Center
Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.
Merck Research Laboratories
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Vanderbilt University Medical Center
Development of N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methyl-4-[11C]methylbenzamide for positron emission tomography imaging of metabotropic glutamate 1 receptor in monkey brain.
National Institute of Radiological Sciences
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.
Sanford-Burnham Medical Research Institute
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Astrazeneca
Synthesis and evaluation of novela-fluorinated (E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyl oxime (ABP688) derivatives as metabotropic glutamate receptor subtype 5 PET radiotracers.
Institute of Technology (Eth) Zurich
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Vanderbilt University Medical Center
Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators.
Lundbeck Research Usa
Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists.
Novartis Institutes For Biomedical Research
N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators.
Lundbeck Research Usa
Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain.
National Institute of Radiological Sciences
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
Vanderbilt University Medical Center
Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().
TBA
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.
Universit£T Leipzig
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.
University of Salerno
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.
Vanderbilt University Medical Center
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Universite Blaise Pascal
Positive and negative modulation of group I metabotropic glutamate receptors.
Institute of Organic Synthesis
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Merck
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.
University of Perugia
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.
University of Perugia
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.
Novartis Institutes For Biomedical Research
A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Astrazeneca R & D M£Lndal
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.
University of Perugia
Ligands for glutamate receptors: design and therapeutic prospects.
The Royal Danish School of Pharmacy
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
Georgetown University Medical Center
(S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors.
Royal Danish School of Pharmacy
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.
Merck Research Laboratories
Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid.
Eli Lilly
Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
Merck Research Laboratories
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkin
Vanderbilt University Medical Center
Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.
Lundbeck Research Usa
6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.
Lundbeck Research Usa
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.
Vanderbilt University Medical Center
Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Schering-Plough Research Institute
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.
Institute For Neurodegenerative Disorders
Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype.
H. Lundbeck
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.
National Institute On Drug Abuse-Intramural Research Program
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.
Vanderbilt University Medical Center
Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.
TBA
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.
Vanderbilt Medical Center
Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Astrazeneca Pharmaceuticals
Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile
TBA
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies.
Pfizer
4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.
Astrazeneca Pharmaceuticals
Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5.
Sepracor
Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands.
Eth Zurich (Swiss Federal Institute of Technology)
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.
Evotec (Uk)
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.
Vanderbilt University Medical Center
Structure-activity relationships of fluorinated (E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with positron emission tomog
Eth Zurich
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
National Institute On Drug Abuse-Intramural Research Program
A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Merck Research Laboratories
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Vanderbilt University Medical Center
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Vanderbilt University Medical Center
Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
Novartis Institutes For Biomedical Research
Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment for psychotic disorders.
Tsukuba Research Institute
Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.
Tsukuba Research Institute
Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.
Merz Pharmaceuticals
Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.
H. Lundbeck
Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonists
TBA
Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC-an apparent mGluR6 selective ligand
TBA
(+)-2-Methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptors
TBA
Synthesis and biology of the rigidified glutamate analogue, trans-2-carboxyazetidine-3-acetic acid (t-CAA)
TBA
Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.
Vanderbilt University Medical Center
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.
National Institute On Drug Abuse-Intramural Research Program
In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.
Medical Research Council Technology
Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Tsukuba Research Institute
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
Vanderbilt University Medical Center
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Pfizer
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Schering-Plough Research Institute
Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.
Pfizer
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Pfizer
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine.
Research Triangle Institute
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Abbott Laboratories
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
National Institute On Drug Abuse
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.
National Institute On Drug Abuse
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
F. Hoffmann-La Roche
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
F. Hoffmann-La Roche
Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Astrazeneca R&D MöLndal
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
Faust Pharmaceuticals
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Abbott Laboratories
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes.
Vanderbilt University School of Medicine
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
National Institute On Drug Abuse
Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.
Nps Pharmaceuticals
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
University of Illinois At Chicago
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists.
F. Hoffmann-La Roche
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.
Astrazeneca R&D
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Abbott Laboratories
3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists.
Merck Research Laboratories
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Merck Research Laboratories
A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone.
Columbia University College of Physicians and Surgeons
Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists.
Merck Research Laboratories
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Merck Research Laboratories
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.
Yale University
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Merck Research Laboratories
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.
Merck Research Laboratories
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Merck Research Laboratories
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Merck Research Laboratories
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Merck Research Laboratories
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
TBA
Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
Taisho Pharmaceutical
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Merck Research Laboratories
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.
Eli Lilly
Discovery and optimization of a novel CNS penetrant series of mGlu
Vanderbilt University
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.
Merck Research Laboratories
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
Centro De Investigaci£N Lilly S.A. Avda. De La Industria
Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid.
The Royal Danish School of Pharmacy
Selective antagonists at group I metabotropic glutamate receptors: synthesis and molecular pharmacology of 4-aryl-3-isoxazolol amino acids.
The Royal Danish School of Pharmacy
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Novartis Pharma
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu
Vanderbilt University
Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.
Bristol-Myers Squibb Research & Development
Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators.
Sumitomo Dainippon Pharma
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu
Vanderbilt University School of Medicine
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.
Recordati
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.
Universit¿A Di Perugia
Surveying heterocycles as amide bioisosteres within a series of mGlu
Vanderbilt University
Cyclobutane quisqualic acid analogues as selective mGluR5a metabotropic glutamic acid receptor ligands.
University of Minnesota
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors
Eli Lilly
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.
Eli Lilly
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist.
Università
(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist.
Eli Lilly
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.
Cresset
Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Vanderbilt University Medical Center
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu
Vanderbilt University School of Medicine
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist.
Università
Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists.
Korea Institute of Science & Technology (Kist)
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.
Eisai
A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core.
Addex Therapeutics
Negative allosteric modulators of metabotropic glutamate receptor subtype.
Dart Neuroscience
The identification of novel orally active mGluR5 antagonist GSK2210875.
Medicines Research Centre
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Vanderbilt University
Isoxazolo[3,4-d]pyridazinones positively modulate the metabotropic glutamate subtypes 2 and 4.
University of Montana
Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu
Gedeon Richter
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Vanderbilt University
Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators.
Sumitomo Dainippon Pharma
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
Vanderbilt University Institute of Imaging Science
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Pfizer
CYCLIC SULFONAMIDE RIBONUCLEOTIDE REDUCTASE (RNR) INHIBITORS AND USES THEREOF
Boundless Bio
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
Pyrazole- and indazole-substituted oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
Boehringer Ingelheim International
Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals
Bayer Animal Health
Methods and compositions for cell-proliferation-related disorders
Agios Pharmaceuticals
Piperidine derivatives for use in the treatment or prevention of psychiatric and neurological conditions
Takeda Pharmaceutical
Inhibitors of the IRE-1/XBP-1 pathway and methods of using thereof
H. Lee Moffitt Cancer Center and Research Institute
Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
Incyte
N-cyclopropyl-N-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
Boehringer Ingelheim International
Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine.
Hebrew University of Jerusalem
Multiheteroaryl compounds as inhibitors of H-PGDS and their use for treating prostaglandin D2 mediated diseases
Cayman Chemical
2-(Hetero(aryl)methylene)hydrazine-1-carbothioamides as potent urease inhibitors.
Quaid-I-Azam University
An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.
Kyushu Institute of Technology
Synthesis of 3,5-disubstituted isoxazolines as protein tyrosine phosphatase 1B inhibitors
Central Drug Research Institute
Biological evaluation and structural determinants of p38α mitogen-activated-protein kinase and c-Jun-N-terminal kinase 3 inhibition by flavonoids.
Eberhard Karls University of Tuebingen
Characterization of the striatal M2 muscarinic receptor mediating inhibition of cyclic AMP using selective antagonists: a comparison with the brainstem M2 receptor.
Abbott Laboratories
Virtual screening for potential inhibitors of homology modeled Leptospira interrogans MurD ligase.
Svims University
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Tufts University
Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy.
University of Illinois
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University of Cambridge
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).
Astrazeneca
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
Synthesis and structure-activity relationships of dehydroaltenusin derivatives as selective DNA polymerase alpha inhibitors.
Kyoto Prefectural University
Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.
Bristol-Myers Squibb