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

Acylglycinamides as inhibitors of glycine transporter type 1.

Glaxosmithkline

Discovery and SAR of org 24598-a selective glycine uptake inhibitor.

Organon Research And Development Group

Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

TBA

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

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

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 GlyT1 inhibitors with improved pharmacokinetic properties.

Merck

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

Discovery and SAR studies of novel GlyT1 inhibitors.

Eli Lilly

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

[3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.

Pfizer

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£

The Druggability of Solute Carriers.

The Scripps Research Institute

Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists.

University Of Eastern Finland

Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.

Astrazeneca

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