The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 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. |
Gedeon Richter |
| 28109949 |
10 |
Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu |
Institute For Advanced Chemistry of Catalonia (Iqac-Csic) |
| 27908761 |
55 |
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache. |
Eli Lilly |
| 27856084 |
54 |
Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential. |
Bristol-Myers Squibb |
| 27836401 |
57 |
Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression. |
Eli Lilly |
| 27994742 |
34 |
Development of 1 |
Bristol-Myers Squibb |
| 26985321 |
54 |
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI. |
Merck Research Laboratories |
| 26985317 |
20 |
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5. |
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. |
Vanderbilt University Medical Center |
| 26810316 |
29 |
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 |
| 26706173 |
13 |
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5. |
Shenyang Pharmaceutical University |
| 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. |
Vanderbilt University Medical Center |
| 26774652 |
12 |
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate. |
Gedeon Richter |
| 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. |
Janssen Pharmaceutica |
| 26475522 |
81 |
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. |
Vanderbilt University Medical Center |
| 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 Selective |
Eli Lilly |
| 26231155 |
53 |
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
Massachusetts General Hospital |
| 26225459 |
48 |
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 |
| 26183084 |
53 |
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound. |
Vanderbilt University Medical Center |
| 26112438 |
31 |
Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators. |
Toray Industries |
| 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. |
University of Modena and Reggio Emilia |
| 22711749 |
1 |
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 |
| 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. |
Korea Institute of Science and Technology |
| 25565255 |
49 |
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 |
| 24969015 |
118 |
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. |
Vanderbilt University Medical Center |
| 24914612 |
36 |
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). |
Vanderbilt University Medical Center |
| 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. |
Pfizer |
| 24147864 |
6 |
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 |
| 24125886 |
40 |
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators. |
Merz Pharmaceuticals |
| 24074843 |
2 |
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. |
Vanderbilt University Medical Center |
| 24050755 |
10 |
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 |
| 24900753 |
25 |
Trisubstituted imidazoles as positive modulators of metabotropic glutamate receptor subtype 5. |
Dart Neuroscience |
| 23947773 |
79 |
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor. |
Janssen Pharmaceutica |
| 23932792 |
74 |
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1. |
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. |
Merz Pharmaceuticals |
| 23770058 |
147 |
Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators. |
Lundbeck Research Usa |
| 23434029 |
55 |
Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators. |
Sk Biopharmaceuticals |
| 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. |
Eli Lilly |
| 23357634 |
74 |
Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators. |
Lundbeck Research Usa |
| 23333207 |
9 |
Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain. |
Brain Science Institute |
| 20483612 |
41 |
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs. |
Gedeon Richter |
| 20005096 |
112 |
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2. |
Glaxosmithkline |
| 18304814 |
105 |
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena. |
Glaxosmithkline |
| 23142615 |
35 |
Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold. |
Vanderbilt University Medical Center |
| 23084894 |
56 |
Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain. |
Merck Research Laboratories |
| 22607673 |
34 |
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 |
| 22533875 |
11 |
Mitigating heterocycle metabolism in drug discovery. |
Amgen |
| 23046966 |
43 |
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
Astrazeneca |
| 22981332 |
58 |
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. |
Vanderbilt University Medical Center |
| 22975301 |
128 |
Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators. |
Lundbeck Research Usa |
| 22963764 |
17 |
Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists. |
Novartis Institutes For Biomedical Research |
| 22832311 |
75 |
N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators. |
Lundbeck Research Usa |
| 22148748 |
23 |
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. |
Vanderbilt University Medical Center |
| 22523618 |
16 |
Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam(). |
TBA |
| 22386665 |
23 |
3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity. |
Eli Lilly |
| 19819046 |
24 |
Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists. |
Universit£T Leipzig |
| 19042134 |
30 |
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands. |
Universit£ |
| 18173231 |
71 |
Positive and negative modulation of group I metabotropic glutamate receptors. |
Institute of Organic Synthesis |
| 17210250 |
45 |
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. |
Merck |
| 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. |
Universit£ |
| 17110115 |
13 |
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 |
| 16839764 |
28 |
A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5). |
Astrazeneca R & D M£Lndal |
| 10893301 |
270 |
Ligands for glutamate receptors: design and therapeutic prospects. |
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. |
Georgetown University Medical Center |
| 7738999 |
88 |
Metabotropic glutamate receptors: novel targets for drug development. |
Cns Research |
| 12565928 |
11 |
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. |
Merck Research Laboratories |
| 9873471 |
111 |
Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid. |
Eli Lilly |
| 22266036 |
116 |
Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain. |
Merck Research Laboratories |
| 21688779 |
84 |
Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. |
Lundbeck Research Usa |
| 21757343 |
73 |
6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators. |
Lundbeck Research Usa |
| 19443219 |
39 |
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. |
Vanderbilt University Medical Center |
| 19433355 |
156 |
Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain. |
Schering-Plough Research Institute |
| 21531137 |
92 |
Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype. |
H. Lundbeck |
| 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. |
Vanderbilt University Medical Center |
| 21315585 |
40 |
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. |
Vanderbilt Medical Center |
| 21295468 |
52 |
Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). |
Astrazeneca Pharmaceuticals |
| 24900255 |
19 |
Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile |
TBA |
| 21067920 |
43 |
4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators. |
Astrazeneca Pharmaceuticals |
| 20965739 |
66 |
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 |
| 20809633 |
16 |
Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5. |
Sepracor |
| 20638279 |
46 |
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. |
Evotec (Uk) |
| 20346665 |
30 |
A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties. |
Merck Research Laboratories |
| 19875287 |
56 |
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. |
Vanderbilt University Medical Center |
| 19931453 |
59 |
Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity. |
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. |
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. |
Tsukuba Research Institute |
| 19443216 |
17 |
Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. |
H. Lundbeck |
| | 13 |
(+)-2-Methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptors |
TBA |
| | 10 |
Synthesis and biology of the rigidified glutamate analogue, trans-2-carboxyazetidine-3-acetic acid (t-CAA) |
TBA |
| 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. |
National Institute On Drug Abuse-Intramural Research Program |
| 19289283 |
34 |
In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists. |
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. |
Tsukuba Research Institute |
| 17929793 |
53 |
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain. |
Schering-Plough Research Institute |
| 17569516 |
14 |
Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. |
Research Triangle Institute |
| 17532216 |
42 |
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists. |
Abbott Laboratories |
| 17336520 |
16 |
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse |
| 17196387 |
38 |
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists. |
F. Hoffmann-La Roche |
| 17189691 |
28 |
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure. |
F. Hoffmann-La Roche |
| 16837196 |
19 |
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 |
| 16809035 |
15 |
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists. |
Abbott Laboratories |
| 16678408 |
32 |
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse |
| 16481165 |
20 |
Structure-activity relationship of thiopyrimidines as mGluR5 antagonists. |
Nps Pharmaceuticals |
| 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. |
University of Illinois At Chicago |
| 16439120 |
28 |
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists. |
F. Hoffmann-La Roche |
| 16380255 |
42 |
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues. |
Astrazeneca R&D |
| 16279797 |
132 |
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. |
Abbott Laboratories |
| 16115767 |
64 |
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. |
Merck Research Laboratories |
| 16039855 |
30 |
Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists. |
Merck Research Laboratories |
| 15686941 |
22 |
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. |
Merck Research Laboratories |
| 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. |
Merck Research Laboratories |
| 15482909 |
60 |
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology. |
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. |
Merck Research Laboratories |
| 15341479 |
36 |
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
TBA |
| 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. |
Merck Research Laboratories |
| 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. |
Merck Research Laboratories |
| 11814808 |
6 |
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5. |
Novartis Pharma |
| 27496211 |
67 |
Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box. |
Bristol-Myers Squibb Research & Development |
| 27432763 |
76 |
Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators. |
Sumitomo Dainippon Pharma |
| 30608678 |
36 |
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu |
Vanderbilt University School of Medicine |
| 30624919 |
502 |
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 |
| 10639281 |
13 |
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity. |
Universit¿A Di Perugia |
| 30910459 |
34 |
Surveying heterocycles as amide bioisosteres within a series of mGlu |
Vanderbilt University |
| 10229632 |
2 |
Cyclobutane quisqualic acid analogues as selective mGluR5a metabotropic glutamic acid receptor ligands. |
University of Minnesota |
| 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 receptors |
Eli Lilly |
| 29939744 |
179 |
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
Shanghaitech University |
| 9873635 |
67 |
2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors. |
Eli Lilly |
| 9873392 |
6 |
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist. |
Università |
| 9871538 |
22 |
(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist. |
Eli Lilly |
| 30807144 |
23 |
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
Cresset |
| 30446311 |
63 |
Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. |
Vanderbilt University Medical Center |
| 30350962 |
102 |
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu |
Vanderbilt University School of Medicine |
| 8709120 |
17 |
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist. |
Università |
| 26598462 |
2 |
Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists. |
Korea Institute of Science & Technology (Kist) |
| 26531152 |
23 |
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 |
| 21051228 |
29 |
The identification of novel orally active mGluR5 antagonist GSK2210875. |
Medicines Research Centre |
| 30180563 |
51 |
Synthesis toward Bivalent Ligands for the Dopamine D |
Ghent University |
| 30143366 |
10 |
Isoxazolo[3,4-d]pyridazinones positively modulate the metabotropic glutamate subtypes 2 and 4. |
University of Montana |
| 29259756 |
32 |
VU6010608, a Novel mGlu |
Vanderbilt University |
| 28390229 |
14 |
Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu |
Gedeon Richter |
| 28838696 |
45 |
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 |
| 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. |
Vanderbilt University Institute of Imaging Science |
| 29350927 |
102 |
Synthesis and Pharmacological Characterization of C4 |
TBA |
| 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. |
Pfizer |
| 28244987 |
10 |
Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11. |
California Institute of Technology |
| 20711197 |
12 |
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery. |
Novartis Institutes For Biomedical Research |
| 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 f |
National Taiwan University |
| 16078847 |
30 |
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. |
Abbott Laboratories |
| 16112583 |
74 |
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
| 9083477 |
11 |
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities. |
Uppsala University |
| 8230098 |
46 |
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships. |
Glaxo Group Research |
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