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134 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review

Article Title
Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment.EBI
Wuxi Apptec (Shanghai)
Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists.EBI
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.EBI
University of Tsukuba
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.EBI
Smithkline Beecham Pharmaceuticals
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.EBI
Merck Research Laboratories
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.EBI
Merck Research Laboratories
Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).EBI
Novartis Institutes For Biomedical Research
Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists.EBI
Kitasato University
Recent trends in orexin research--2010 to 2015.EBI
Actelion Pharmaceuticals
Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.EBI
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.EBI
Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.EBI
Merck Research Laboratories
Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.EBI
Actelion Pharmaceuticals
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.EBI
Merck Research Laboratories
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.EBI
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.EBI
Merck Research Laboratories
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.EBI
Merck Research Laboratories
Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.EBI
Merck Research Laboratories
Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1.EBI
Actelion Pharmaceuticals
Truncated Orexin Peptides: Structure-Activity Relationship Studies.EBI
Research Triangle Institute
Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).EBI
Merck Research Laboratories
Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia.EBI
Novartis Institutes For Biomedical Research
Synthesis and evaluation of novel radioligands for positron emission tomography imaging of the orexin-2 receptor.EBI
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.EBI
Research Triangle Institute
Selective orexin receptor antagonists.EBI
Janssen Pharmaceutica
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.EBI
Actelion Pharmaceuticals
Radiosynthesis and evaluation of [11C]EMPA as a potential PET tracer for orexin 2 receptors.EBI
Harvard Medical School
Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.EBI
Actelion Pharmaceuticals
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.EBI
Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies.EBI
Research Triangle Institute
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.EBI
Scripps Florida
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.EBI
Merck Research Laboratories
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.EBI
Merck Research Laboratories
Proline bis-amides as potent dual orexin receptor antagonists.EBI
Merck Research Laboratories
Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists.EBI
Takeda Pharmaceutical
Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists.EBI
Takeda Pharmaceutical
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.EBI
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.EBI
Merck Research Laboratories
Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.EBI
Actelion Pharmaceuticals
N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.EBI
Actelion Pharmaceuticals
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.EBI
Actelion Pharmaceuticals
Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding.EBI
Merck Research Laboratories
Discovery of orexin 2 receptor selective and dual orexin receptor agonists based on the tetralin structure: Switching of receptor selectivity by chirality on the tetralin ring.EBI
University of Tsukuba
Essential structure of orexin 1 receptor antagonist YNT-707: Conversion of the 16-cyclopropylmethyl group to the 16-sulfonamide group in d-nor-nalfurafine derivatives.EBI
University of Tsukuba
Design and synthesis of novel orexin 2 receptor agonists based on naphthalene skeleton.EBI
University of Tsukuba
Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.EBI
University of Tsukuba
Discovery of novel orexin receptor antagonists using a 1,3,5-trioxazatriquinane bearing multiple effective residues (TriMER) library.EBI
University of Tsukuba
Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.EBI
Takeda Pharmaceutical
Discovery of Arylsulfonamides as Dual Orexin Receptor Agonists.EBI
Research Triangle Institute
Structure-activity studies of orexin a and orexin B at the human orexin 1 and orexin 2 receptors led to orexin 2 receptor selective and orexin 1 receptor preferring ligands.EBI
University of Leipzig
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.EBI
Banyu Tsukuba Research Institute
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.EBI
Janssen Research & Development
Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.EBI
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.EBI
Banyu Tsukuba Research Institute
Antagonists of Orexin Receptors as Potential Treatment of Sleep Disorders, Obesity, Eating Disorders, and Other Neurological and Psychiatric Disorders.EBI
Therachem Research Medilab (India)
Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia.EBI
Taisho Pharmaceutical
Essential structure of orexin 1 receptor antagonist YNT-707, part V: Structure-activity relationship study of the substituents on the 17-amino group.EBI
University of Tsukuba
Pharmacophore Model To Discover OX1 and OX2 Orexin Receptor Ligands.EBI
University of Helsinki
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.EBI
Essential structure of orexin 1 receptor antagonist YNT-707, part III: Role of the 14-hydroxy and the 3-methoxy groups in antagonistic activity toward the orexin 1 receptor in YNT-707 derivatives lacking the 4,5-epoxy ring.EBI
University of Tsukuba
Essential structure of orexin 1 receptor antagonist YNT-707, Part IV: The role of D-ring in 4,5-epoxymorphinan on the orexin 1 receptor antagonistic activity.EBI
University of Tsukuba
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.EBI
Sosei Heptares
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.EBI
Johnson and Johnson Pharmaceutical Research and Development
Azulene-based compounds for targeting orexin receptors.EBI
University of Helsinki
Essential structure of orexin 1 receptor antagonist YNT-707, Part II: Drastic effect of the 14-hydroxy group on the orexin 1 receptor antagonistic activity.EBI
University of Tsukuba
Essential structure of orexin 1 receptor antagonist YNT-707, Part I: Role of the 4,5-epoxy ring for binding with orexin 1 receptor.EBI
University of Tsukuba
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide.EBI
Taisho Pharmaceutical
Glutathione transferase from Plasmodium falciparum--interaction with malagashanine and selected plant natural products.BDB
University of Zimbabwe
Conferin, potent antioxidant and anti-inflammatory isoflavone from Caragana conferta Benth.BDB
University of Karachi
An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms.BDB
Universitätsklinikum Frankfurt
Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.BDB
University of North Carolina
Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.BDB
Merck Research Laboratories
A(3) adenosine receptors in human neutrophils and promyelocytic HL60 cells: a pharmacological and biochemical study.BDB
University of Ferrara
Cloned human and rat galanin GALR3 receptors. Pharmacology and activation of G-protein inwardly rectifying K+ channels.BDB
Synaptic Pharmaceutical
SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.BDB
Smithkline Beecham Pharmaceuticals
Pharmacokinetic/pharmacodynamic relationship of benzodiazepines in the direct cortical stimulation model of anticonvulsant effect.BDB
Leiden University
Structural combination of established 5-HT(2A) receptor ligands: new aspects of the binding mode.BDB
University of Mainz
A new screening assay for allosteric inhibitors of cSrc.BDB
Chemical Genomics Centre of The Max Planck Society
Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: quinone oxidoreductase-1 (NQO1).BDB
University of Manchester
Tetraiodobenzimidazoles are potent inhibitors of protein kinase CK2.BDB
University of Padova
5,6-Dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.BDB
Anadys Pharmaceuticals
Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins.BDB
Sapienza University of Rome
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.BDB
Abbott Laboratories
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.BDB
Bristol-Myers Squibb
Selectivity determinants of inhibitor binding to human 20alpha-hydroxysteroid dehydrogenase: crystal structure of the enzyme in ternary complex with coenzyme and the potent inhibitor 3,5-dichlorosalicylic acid.BDB
Monash University
Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid.BDB
Universita Degli Studi Di Firenze
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.BDB
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.BDB
Wyeth Research
Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors.BDB
Enantiospecificity of glutamate carboxypeptidase II inhibition.BDB
Guilford Pharmaceuticals
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.BDB
National Institutes of Health
Phylogenomic Analysis of the Microviridin Biosynthetic Pathway Coupled with Targeted Chemo-Enzymatic Synthesis Yields Potent Protease Inhibitors.BDB
University of Helsinki
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.BDB
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.BDB
Merck Research Laboratories
High-resolution crystal structure of aldose reductase complexed with the novel sulfonyl-pyridazinone inhibitor exhibiting an alternative active site anchoring group.BDB
Philipps University Marburg