58 articles for thisTarget
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PMID
Data
Article Title
Organization
3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.
F. Hoffmann-La Roche
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres.
Vanderbilt University Medical Center
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead.
Vanderbilt University Medical Center
The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities.
Drexel University College of Medicine
Atropisomeric 4-phenyl-4H-1,2,4-triazoles as selective glycine transporter 1 inhibitors.
Astellas Pharma
Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1.
Amri
1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.
Glaxosmithkline
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Organon Research and Development Group
Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors.
Astellas Pharma
Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.
F. Hoffmann-La Roche
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Merck And
4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.
F. Hoffmann-La Roche
5,5-Diaryl-2-amino-4-pentenoates as novel, potent, and selective glycine transporter type-2 reuptake inhibitors.
Nps Pharmaceuticals
Synthesis and characterization of [¹²¿?¿I]2-iodo N-[(S)-{(S)-1-methylpiperidin-2-yl}(phenyl)methyl]3-trifluoromethyl-benzamide as novel imaging probe for glycine transporter 1.
Nagasaki University
Synthesis and biological evaluation of (4H-1,2,4-triazol-4-yl)isoquinoline derivatives as selective glycine transporter 1 inhibitors.
Astellas Pharma
Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.
F. Hoffmann-La Roche
An octahydro-cyclopenta[c]pyrrole series of inhibitors of the type 1 glycine transporter.
Pfizer
The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter.
Pfizer
Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
Merck Sharp and Dohme Research Laboratories
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Merck
Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
F. Hoffmann-La Roche
Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.
F. Hoffmann-La Roche
A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening.
Pfizer
Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.
F. Hoffmann-La Roche
Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.
F. Hoffmann-La Roche
The synthesis and SAR of 2-arylsulfanylphenyl-1-oxyalkylamino acids as GlyT-1 inhibitors.
H. Lundbeck
Sarcosine based indandione hGlyT1 inhibitors.
Merck Sharp and Dohme Research Laboratories
Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
F. Hoffmann-La Roche
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.
F. Hoffmann-La Roche
The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors.
H. Lundbeck
The first potent and selective inhibitors of the glycine transporter type 2.
Organon Laboratories
Azetidine-based selective glycine transporter-1 (GlyT1) inhibitors with memory enhancing properties.
Dart Neuroscience
Development of an N-Acyl Amino Acid That Selectively Inhibits the Glycine Transporter 2 To Produce Analgesia in a Rat Model of Chronic Pain.
University of Sydney
Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations.
The University of Texas At El Paso
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1.
Amri
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists.
University of Eastern Finland
Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain.
Albany College of Pharmacy and Health Sciences
Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.
Dart Neuroscience
Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Abbvie Deutschland
De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors.
Abbvie
The structural basis for the interaction between L-tryptophan and the Escherichia coli trp aporepressor.
University of Chicago
Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L.
Epizyme
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach.
University of Bonn
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
Northwestern University
Binding of selective antagonists to four muscarinic receptors (M1 to M4) in rat forebrain.
UniversitÉ
Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors.
University of Luxembourg