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98 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27908761 55 Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.EBI Eli Lilly and Company
27836401 57 Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.EBI Eli Lilly and Company
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
26988302 104 Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.EBI Vanderbilt University Medical Center
26778256 145 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.EBI Vanderbilt University Medical Center
26684851 86 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.EBI Janssen Pharmaceutica NV
26476971 117 Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.EBI Vanderbilt University Medical Center
26475522 81 Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.EBI Vanderbilt University Medical Center
26426481 114 Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in SchizophrenicsEBI Vanderbilt University
26313429 155 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 SelectiveEBI Eli Lilly and Company
26231155 53 Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.EBI Massachusetts General Hospital
25638496 2 GPCR crystal structures: Medicinal chemistry in the pocket.EBI Friedrich-Alexander University
25984841 19 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.EBI Korea Institute of Science and Technology
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
25127154 24 Novel thienopyrimidinones as mGluR1 antagonists.EBI Yonsei University
24392688 31 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.EBI Pfizer Inc
23947773 79 Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.EBI Janssen Pharmaceutica NV
23932792 74 Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.EBI Vanderbilt University Medical Center
23856046 41 Discovery, synthesis, and structure-activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators.EBI Merz Pharmaceuticals GmbH
23727046 84 N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.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
17157010 8 13C bis-labeled pyrroles: a tool for the identification of the rat metabolism of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester.EBI GlaxoSmithKline
20817521 21 A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.EBI Merck Research Laboratories
20005096 112 The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.EBI GlaxoSmithKline
23084894 56 Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.EBI Merck Research Laboratories
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
22981332 58 Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.EBI Vanderbilt University Medical Center
22148748 23 Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.EBI Vanderbilt University Medical Center
22386665 23 3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity.EBI Eli Lilly and Company
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
19042134 30 Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.EBI Universit£ di Salerno
17489573 16 Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.EBI Eli Lilly and Company
17725337 40 Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.EBI Universit£ di Perugia
16839764 28 A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).EBI AstraZeneca R & D M£lndal
15771457 77 Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.EBI Janssen-Cilag S.A.
10893301 270 Ligands for glutamate receptors: design and therapeutic prospects.EBI The Royal Danish School of Pharmacy
9572889 39 Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.EBI Georgetown University Medical Center
8759641 48 A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.EBI Royal Danish School of Pharmacy
7738999 88 Metabotropic glutamate receptors: novel targets for drug development.EBI CNS Research
10673095 2 First enantiospecific synthesis of a 3,4-dihydroxy-L-glutamic acid [(3S,4S)-DHGA], a new mGluR1 agonist.EBI CNRS
9873471 111 Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid.EBI Eli Lilly and Company
22266036 116 Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.EBI Merck Research Laboratories
21688779 84 Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.EBI Lundbeck Research USA, Inc.
19443219 39 Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.EBI Vanderbilt University Medical Center
19433355 156 Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.EBI Schering-Plough Research Institute
21470858 4 Radiosynthesis and preliminary evaluation of 4-[18F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1.EBI National Institute of Radiological Sciences
24900255 19 Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK ProfileEBI TBA
21172734 7 Synthesis and evaluation of 6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain.EBI National Institute of Radiological Sciences
20873775 18 Assessment of structurally diverse philanthotoxin analogues for inhibitory activity on ionotropic glutamate receptor subtypes: discovery of nanomolar, nonselective, and use-dependent antagonists.EBI University of Copenhagen
20638290 9 A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity.EBI The University of Adelaide
20615697 49 Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.EBI Gedeon Richter Plc
20346665 30 A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.EBI Merck Research Laboratories
19931453 59 Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.EBI Novartis Institutes for BioMedical Research
19692242 30 Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment for psychotic disorders.EBI Tsukuba Research Institute
19674894 34 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.EBI Tsukuba Research Institute
19574055 82 Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1.EBI Merz Pharmaceuticals GmbH
 13 (+)-2-Methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptorsEBI TBA
 5 A novel class of antagonists for metabotropic glutamate receptors, 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylatesEBI TBA
 10 Synthesis and biology of the rigidified glutamate analogue, trans-2-carboxyazetidine-3-acetic acid (t-CAA)EBI TBA
 2 Synthesis of conformationally-constrained stereospecific analogs of glutamic acid as antagonists of metabotropic receptorsEBI 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
19289283 34 In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists.EBI Medical Research Council Technology
18849168 48 Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.EBI Tsukuba Research Institute
17929793 53 Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.EBI Schering-Plough Research Institute
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
17532216 42 Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.EBI Abbott Laboratories
16809035 15 Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.EBI Abbott Laboratories
16392801 8 Rational design and enantioselective synthesis of (1R,4S,5R,6S)-3-azabicyclo[3.3.0]octane-4,6-dicarboxylic acid - a novel inhibitor at human glutamate transporter subtypes 1, 2, and 3.EBI The Danish University of Pharmaceutical Sciences
16279797 132 Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.EBI Abbott Laboratories
12747796 39 Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).EBI The Danish University of Pharmaceutical Sciences
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
32173198 58 Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.EBI Merck & Co.
11087567 6 Chiral resolution, pharmacological characterization, and receptor docking of the noncompetitive mGlu1 receptor antagonist (+/-)-2-hydroxyimino- 1a, 2-dihydro-1H-7-oxacyclopropa[b]naphthalene-7a-carboxylic acid ethyl ester.EBI Novartis Pharma AG
30608678 36 Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGluEBI Vanderbilt University School of Medicine
10639281 13 Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.EBI Universit¿a di Perugia
31789518 11 Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.EBI Purdue University
30910459 34 Surveying heterocycles as amide bioisosteres within a series of mGluEBI Vanderbilt University
10090786 33 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 receptorsEBI Eli Lilly and Company
9873635 67 2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.EBI Eli Lilly and Company
9873392 6 Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist.EBI Università degli Studi
9871538 22 (2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist.EBI Eli Lilly and Company
9301676 14 Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.EBI Université René Descartes-Paris V
30350962 102 Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGluEBI Vanderbilt University School of Medicine
8831765 9 Homology modeling of metabotropic glutamate receptors. (mGluRs) structural motifs affecting binding modes and pharmacological profile of mGluR1 agonists and competitive antagonists.EBI Università di Perugia
8709120 17 (S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist.EBI Università di Perugia
27013388 44 Re-exploration of the mGlu? PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.EBI Vanderbilt University Medical Center
8667369 121 Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2'-carboxy-3'-phenylcyclopropyl)glycine. Focus on (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptors antagonist.EBI Università di Perugia
7562903 10 1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors.EBI Università di Perugia
29259756 32 VU6010608, a Novel mGluEBI Vanderbilt University
29350927 102 Synthesis and Pharmacological Characterization of C4EBI TBA
18393401 70 Design and Synthesis of 2- and 3-Substituted-3-phenylpropyl Analogs of 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: Role of Amino, Fluoro, Hydroxyl, Methoxyl, Methyl, Methylene, and Oxo Substituents on Affinity fBDB National Taiwan University