125 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1.
Shionogi
Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2.
Shionogi
Discovery of imidazo[1,2-b]pyridazine derivatives: selective and orally available Mps1 (TTK) kinase inhibitors exhibiting remarkable antiproliferative activity.
Shionogi
Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125).
Shionogi
Design, synthesis, and binding mode prediction of 2-pyridone-based selective CB2 receptor agonists.
Shionogi
Identification of a novel benzimidazole derivative as a highly potent NPY Y5 receptor antagonist with an anti-obesity profile.
Shionogi
Conformational restriction approach toß-secretase (BACE1) inhibitors: effect of a cyclopropane ring to induce an alternative binding mode.
Shionogi
Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy.
Shionogi
Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles.
Shionogi
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.
Shionogi
CB 1/2 dual agonists with 3-carbamoyl 2-pyridone derivatives as antipruritics: reduction of CNS side effects by introducing polar functional groups.
Shionogi
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
Shionogi
Identification of glycosylated exendin-4 analogue with prolonged blood glucose-lowering activity through glycosylation scanning substitution.
Shionogi
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs.
Shionogi
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.
Shionogi
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.
Shionogi
Design, Synthesis, and Anti-Inflammatory Evaluation of a Novel PPARδ Agonist with a 4-(1-Pyrrolidinyl)piperidine Structure.
Shionogi
Discovery and structure-activity relationship study of 2-piperazinyl-benzothiazole derivatives as potent and selective PPARδ agonists.
Shionogi
A Quantum Mechanics-Based Method to Predict Intramolecular Hydrogen Bond Formation Reflecting P-glycoprotein Recognition.
Shionogi
Identification of novel benzimidazole derivatives as highly potent AMPK activators with anti-diabetic profiles.
Shionogi
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.
Shionogi
Identification of novel indole derivatives as highly potent AMPK activators with anti-diabetic profiles.
Shionogi
Peptide-to-Small Molecule: A Pharmacophore-Guided Small Molecule Lead Generation Strategy from High-Affinity Macrocyclic Peptides.
Shionogi
Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
Shionogi
Highly Potent and Oral Macrocyclic Peptides as a HIV-1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization.
Shionogi
Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Shionogi
Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Shionogi
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2.
Shionogi
Balancing potency and basicity by incorporating fluoropyridine moieties: Discovery of a 1-amino-3,4-dihydro-2,6-naphthyridine BACE1 inhibitor that affords robust and sustained central Aβ reduction.
Shionogi
Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell.
Shionogi
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives.
Shionogi
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.
Shionogi
Structure-activity relationships of a novel class of endothelin-A receptor antagonists and discovery of potent and selective receptor antagonist, 2-(benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4-(4-methoxyphenyl)-2H-chromene-3-carboxylic acid (S-1255). 1. Study on structure-activity relationships and bas
Shionogi
Discovery of a benzimidazole series as the first highly potent and selective ACSL1 inhibitors.
Shionogi
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 3: Structure-activity relationships of pyrropyrazolone derivatives.
Shionogi
Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.
Shionogi
Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'.
Shionogi
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Shionogi
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
Shionogi
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Shionogi
1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists.
Shionogi
Homology modeling of gelatinase catalytic domains and docking simulations of novel sulfonamide inhibitors.
Shionogi
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.
Shionogi
Synthesis and SAR Study of Carbamoyl Pyridone Bicycle Derivatives as Potent Inhibitors of Influenza Cap-dependent Endonuclease.
Shionogi
Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.
Shionogi
Discovery of NR2B-selective antagonists via scaffold hopping and pharmacokinetic profile optimization.
Shionogi
Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects.
Shionogi
Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives.
Shionogi
Selective CB2 agonists with anti-pruritic activity: discovery of potent and orally available bicyclic 2-pyridones.
Shionogi
Conformational restriction approach to BACE1 inhibitors II: SAR study of the isocytosine derivatives fixed with a cis-cyclopropane ring.
Shionogi
Novel angiotensin II receptor antagonists. Design, synthesis, and in vitro evaluation of dibenzo[a,d]cycloheptene and dibenzo[b,f]oxepin derivatives. Searching for bioisosteres of biphenylyltetrazole using a three-dimensional search technique.
Shionogi
Carbamoyl pyridone HIV-1 integrase inhibitors. 1. Molecular design and establishment of an advanced two-metal binding pharmacophore.
Shionogi
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.
Shionogi
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.
Shionogi
Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003.
Shionogi
Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy.
Shionogi
Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid.
Shionogi
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.
Shionogi
Discovery of orally bioavailable cyclohexanol-based NR2B-selective NMDA receptor antagonists with analgesic activity utilizing a scaffold hopping approach.
Shionogi
Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain.
Shionogi
TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
Genentech
7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds as gamma- secretase modulators for the treatment of alzheimer's disease
Hoffmann-La Roche
ARYL HETEROCYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
D.E. Shaw Research
[9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11BH-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto
Neurocrine Biosciences
Methods to determine KDM1A target engagement and chemoprobes useful therefor
Oryzon Genomics
Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.
National Institutes of Health
1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
Astrazeneca
S-substituted quinazolines and their therapeutic applications for the treatment of diseases mediated by PDE7
Consejo Superior De Investigaciones Cientificas
Synthesis and antiproliferative activities against Hep-G2 of salicylanide derivatives: potent inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase.
Nanjing University
Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives.
Warsaw University of Technology
Synthesis, characterization and biological evaluation of novel chalcone sulfonamide hybrids as potent intestinal alkaline phosphatase inhibitors.
Comsats Institute of Information Technology
Electrostatic Control of Isoform Selective Inhibitor Binding in Nitric Oxide Synthase.
University of California Irvine
mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl) ureas as p38 MAP kinase inhibitors
Respivert
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.
Vanderbilt University
Identification and Co-complex Structure of a New S. pyogenes SpeB Small Molecule Inhibitor.
The Scripps Research Institute
Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
Galderma Research & Development
Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons.
State University of New York
Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.
Washington University
Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family.
Novo Nordisk
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
UniversitÄT Heidelberg