The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27777004 |
90 |
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 |
27774122 |
8 |
Protease-Activated Receptor 1 (PAR-1) Antagonists as Potential Treatment for Acute Coronary Syndrome. |
Therachem Research Medilab (India) |
27075367 |
55 |
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2. |
Bayer Pharma |
25937878 |
9 |
The chemistry and pharmacology of privileged pyrroloquinazolines. |
Oregon Health & Science University |
25176330 |
14 |
Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. |
Northwest Agriculture & Forestry University |
24900880 |
12 |
Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar. |
Merck Research Laboratories |
24900795 |
22 |
Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar. |
Merck Research Laboratories |
24900604 |
40 |
Discovery of Octahydroindenes as PAR1 Antagonists. |
Korea Research Institute of Technology |
23895492 |
49 |
Toward drugs for protease-activated receptor 2 (PAR2). |
The University of Queensland |
22408714 |
23 |
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. |
TBA |
22405832 |
24 |
Discovery of nor-seco himbacine analogs as thrombin receptor antagonists. |
Pfizer |
8960546 |
160 |
Development of potent thrombin receptor antagonist peptides. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
9873407 |
27 |
Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif. |
R. W. Johnson Pharmaceutical Research Institute |
20888225 |
17 |
Discovery of a vorapaxar analog with increased aqueous solubility. |
Merck Research Laboratories |
7673943 |
1 |
Aplysillin A, a Thrombin Receptor Antagonist from the Marine Sponge Aplysina fistularis fulva |
TBA |
| 54 |
Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042 |
TBA |
18447380 |
28 |
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. |
Schering-Plough Research Institute |
17854166 |
33 |
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists. |
Schering-Plough Research Institute |
17574850 |
27 |
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring. |
Schering-Plough Research Institute |
17490877 |
30 |
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core. |
Schering-Plough Research Institute |
17201416 |
24 |
Metabolism-based identification of a potent thrombin receptor antagonist. |
Schering-Plough Research Institute |
16824760 |
22 |
Himbacine derived thrombin receptor (PAR-1) antagonists: structure-activity relationship of the lactone ring. |
Schering-Plough Research Institute |
16380251 |
31 |
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists. |
Schering-Plough Research Institute |
16161991 |
50 |
Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. |
Schering-Plough Research Institute |
12798334 |
18 |
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 |
11814787 |
73 |
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1). |
Merck Research Laboratories |
11597414 |
10 |
Potent, low molecular weight thrombin receptor antagonists. |
Schering-Plough Research Institute |
11591503 |
7 |
Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists. |
Merck Research Laboratories |
11514149 |
86 |
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 |
32122739 |
6 |
Design and synthesis of potent PAR-1 antagonists based on vorapaxar. |
Hebei University of Technology |
11297447 |
18 |
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 |
27482618 |
64 |
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 ?-Thrombin. |
Northwest Agriculture & Forestry University |
31246024 |
106 |
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy. |
Bristol-Myers Squibb Research & Development |
10450984 |
16 |
Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists. |
Schering-Plough Research Institute |
10360749 |
97 |
Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1). |
The R. W. Johnson Pharmaceutical Research Institute |
10230630 |
36 |
Thrombin inhibitors based on a propargylglycine template. |
Biotech Research Institute |
10021945 |
8 |
Photoactivatable peptides based on BMS-197525: a potent antagonist of the human thrombin receptor (PAR-1). |
University At Stony Brook |
31320211 |
15 |
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability. |
Marquette University |
30655958 |
20 |
Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization. |
Marquette University |
29457894 |
4 |
Small Molecule Allosteric Modulators of G-Protein-Coupled Receptors: Drug-Target Interactions. |
Shanghai Jiao Tong University |
7562949 |
61 |
Development of a potent thrombin receptor ligand. |
Merck Research Laboratories |
29685684 |
20 |
Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells. |
Marquette University |
28745507 |
49 |
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide. |
Shandong University |
10471378 |
4 |
6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties. |
Instituto De BiologÍA Celular |
16949284 |
34 |
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors. |
Johnson & Johnson Pharmaceutical |