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125 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28212015 51 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.EBI Gedeon Richter Plc
28109949 10 Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGluEBI Institute for Advanced Chemistry of Catalonia (IQAC-CSIC)
27994742 34 Development of 1EBI Bristol-Myers Squibb Co.
26985317 20 Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.EBI Bristol-Myers Squibb Research & Development
26988308 130 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.EBI Vanderbilt University Medical Center
26814576 146 New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III.EBI University of Copenhagen
26706173 13 7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5.EBI Shenyang Pharmaceutical University
26774652 12 4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.EBI Gedeon Richter Plc
26516782 59 Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.EBI University of Copenhagen
26475522 81 Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.EBI Vanderbilt University Medical Center
26335039 320 Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.EBI Vanderbilt University Medical Center
26014480 87 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.EBI University of Modena and Reggio Emilia
25958247 22 Synthesis and studies on the mGluR agonist activity of FAP4 stereoisomers.EBI Univ. Rouen
25791451 126 Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization.EBI Gedeon Richter Plc
25683622 86 Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).EBI Janssen Pharmaceutica NV
25017030 17 Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization.EBI Gedeon Richter Plc
24969015 118 Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.EBI Vanderbilt University Medical Center
24961642 82 Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.EBI Vanderbilt University Medical Center
24914612 36 Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).EBI Vanderbilt University Medical Center
23374867 40 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.EBI Eli Lilly and Company
22924094 41 Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.EBI TBA
20732812 118 3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators.EBI Vanderbilt University
20483612 41 Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.EBI Gedeon Richter Plc
23142615 35 Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold.EBI Vanderbilt University Medical Center
22607673 34 Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.EBI Vanderbilt University Medical Center
23194448 9 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.EBI National Institute of Radiological Sciences
23009245 53 Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.EBI Sanford-Burnham Medical Research Institute
23046966 43 Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.EBI AstraZeneca
22822714 6 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.EBI Institute of Technology (ETH) Zurich
22981332 58 Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.EBI Vanderbilt University Medical Center
22316010 12 Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain.EBI National Institute of Radiological Sciences
21207959 69 Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI National Institute of Mental Health
18793851 4 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.EBI Vanderbilt University Medical Center
18578478 60 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.EBI Universite Blaise Pascal
18173231 71 Positive and negative modulation of group I metabotropic glutamate receptors.EBI Institute of Organic Synthesis
17210250 45 Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.EBI Merck & Co.
17350267 48 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.EBI Universit£ di Perugia
17110115 13 ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies.EBI Novartis Institutes for BioMedical Research
16213710 32 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.EBI Universit£ di Perugia
9357538 38 (S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors.EBI Royal Danish School of Pharmacy
7738999 88 Metabotropic glutamate receptors: novel targets for drug development.EBI CNS Research
12565928 11 [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.EBI Merck Research Laboratories
21966889 61 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 antiparkinEBI Vanderbilt University Medical Center
21546249 42 Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.EBI Institute for Neurodegenerative Disorders
21295978 22 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.EBI National Institute on Drug Abuse-Intramural Research Program
21183344 59 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.EBI Vanderbilt University Medical Center
23308336 13 Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.EBI TBA
24900255 19 Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK ProfileEBI TBA
21126874 38 3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies.EBI Pfizer Inc
20809633 16 Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5.EBI Sepracor Inc.
20634080 4 Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands.EBI ETH Zurich (Swiss Federal Institute of Technology)
20638279 46 An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.EBI Evotec (UK) Ltd
20615697 49 Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.EBI Gedeon Richter Plc
20598884 48 3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.EBI Vanderbilt University Medical Center
20411954 17 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 tomogEBI ETH Zurich
20382541 31 Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.EBI National Institute on Drug Abuse-Intramural Research Program
20346665 30 A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.EBI Merck Research Laboratories
19875287 56 Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.EBI Vanderbilt University Medical Center
19854049 49 Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.EBI Vanderbilt University Medical Center
19931453 59 Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.EBI Novartis Institutes for BioMedical Research
19574055 82 Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.EBI Merz Pharmaceuticals GmbH
 6 Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonistsEBI TBA
 15 Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC-an apparent mGluR6 selective ligandEBI TBA
19537763 24 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.EBI Vanderbilt University Medical Center
19445453 87 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.EBI National Institute on Drug Abuse-Intramural Research Program
18550372 14 Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.EBI Vanderbilt University Medical Center
17936624 30 Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.EBI Pfizer Inc
17723296 23 Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists.EBI Pfizer Inc
17590335 39 Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.EBI Pfizer Inc
17571866 49 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.EBI National Institute of Mental Health
17446071 15 Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.EBI National Institute on Drug Abuse
17336520 16 Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.EBI National Institute on Drug Abuse
16828551 12 Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.EBI Faust Pharmaceuticals
16809035 15 Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.EBI Abbott Laboratories
16722652 95 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.EBI Vanderbilt University School of Medicine
16678408 32 Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.EBI National Institute on Drug Abuse
16451073 63 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.EBI University of Illinois at Chicago
16380255 42 Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.EBI AstraZeneca R&D
16279797 132 Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.EBI Abbott Laboratories
16183275 42 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists.EBI Merck Research Laboratories
16115767 64 Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.EBI Merck Research Laboratories
16078827 2 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.EBI Columbia University College of Physicians and Surgeons
15686891 45 Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.EBI Yale University
15537338 38 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.EBI Merck Research Laboratories
15482908 13 Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.EBI Merck Research Laboratories
15482907 36 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.EBI Merck Research Laboratories
15482906 25 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.EBI Merck Research Laboratories
15341479 36 Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.EBI TBA
15317467 105 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.EBI Taisho Pharmaceutical Co., Ltd
15225713 36 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.EBI Merck Research Laboratories
14711315 72 (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.EBI Eli Lilly and Company
14643338 124 Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI Virginia Commonwealth University
12825948 13 Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.EBI Università degli Studi di Milano
12519057 22 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.EBI Merck Research Laboratories
12213064 33 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.EBI The Royal Danish School of Pharmacy
11831912 43 Selective antagonists at group I metabotropic glutamate receptors: synthesis and molecular pharmacology of 4-aryl-3-isoxazolol amino acids.EBI The Royal Danish School of Pharmacy
31789518 11 Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.EBI Purdue University
29939744 179 Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.EBI ShanghaiTech University
23850200 36 A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core.EBI Addex Therapeutics
24900698 4 Negative allosteric modulators of metabotropic glutamate receptor subtype.EBI Dart Neuroscience LLC
29705142 58 Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.EBI Vanderbilt University
29057060 100 Discovery of VU6005649, a CNS Penetrant mGluEBI Vanderbilt University
28947938 63 Design and Synthesis of EBI Vanderbilt University School of Medicine
28390229 14 Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGluEBI Gedeon Richter Plc
28958625 88 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.EBI Vanderbilt University
28530802 121 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.EBI Vanderbilt University Institute of Imaging Science
28817277 34 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.EBI Pfizer Inc
28244987 10 Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.BDB California Institute of Technology
26010139 34 Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety.BDB Tehran University of Medical Sciences
11071707 71 Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin.BDB NIH
28425720 3 A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.BDB Celgene Corporation
10514285 66 Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.BDB Medivir AB