53 articles for thisTarget
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Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles.
Vanderbilt University Medical Center
Protease-Activated Receptor 1 (PAR-1) Antagonists as Potential Treatment for Acute Coronary Syndrome.
Therachem Research Medilab (India)
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Bayer Pharma
The chemistry and pharmacology of privileged pyrroloquinazolines.
Oregon Health & Science University
Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Northwest Agriculture & Forestry University
Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar.
Merck Research Laboratories
Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar.
Merck Research Laboratories
Discovery of Octahydroindenes as PAR1 Antagonists.
Korea Research Institute of Technology
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
TBA
Development of potent thrombin receptor antagonist peptides.
Bristol-Myers Squibb Pharmaceutical Research Institute
Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.
R. W. Johnson Pharmaceutical Research Institute
Discovery of a vorapaxar analog with increased aqueous solubility.
Merck Research Laboratories
Aplysillin A, a Thrombin Receptor Antagonist from the Marine Sponge Aplysina fistularis fulva
TBA
Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042
TBA
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Schering-Plough Research Institute
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.
Schering-Plough Research Institute
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.
Schering-Plough Research Institute
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.
Schering-Plough Research Institute
Metabolism-based identification of a potent thrombin receptor antagonist.
Schering-Plough Research Institute
Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring.
Schering-Plough Research Institute
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.
Schering-Plough Research Institute
Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents.
Schering-Plough Research Institute
Direct evidence of edge-to-face CH/π interaction for PAR-1 thrombin receptor activation.
Kyushu University
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
TBA
Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold.
China Pharmaceutical University
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.
Johnson & Johnson Pharmaceutical Research & Development
Protease activated receptor 4 (PAR4) antagonists: Research progress on small molecules in the field of antiplatelet agents.
China Pharmaceutical University
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).
Merck Research Laboratories
Potent, low molecular weight thrombin receptor antagonists.
Schering-Plough Research Institute
Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.
Merck Research Laboratories
Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.
The R. W. Johnson Pharmaceutical Research Institute
Design and synthesis of potent PAR-1 antagonists based on vorapaxar.
Hebei University of Technology
Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.
The R. W. Johnson Pharmaceutical Research Institute
Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin.
Northwest Agriculture & Forestry University
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Bristol-Myers Squibb Research & Development
Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.
Schering-Plough Research Institute
Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).
The R. W. Johnson Pharmaceutical Research Institute
Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1).
University At Stony Brook
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.
Marquette University
Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization.
Marquette University
Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug-Target Interactions.
Shanghai Jiao Tong University
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.
Marquette University
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide.
Shandong University
Evaluation of 2-indolcarbohydrazones as potent a-glucosidase inhibitors, in silico studies and DFT based stereochemical predictions.
Universiti Teknologi Mara (Uitm)
Piperidinyl derivative as a modulator of chemokine receptor activity
Bristol-Myers Squibb
OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
Second Tokushima Institute of New Drug Research