82 articles for thisTarget
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Article Title
Organization
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.
Bristol-Myers Squibb Research & Development
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.
Southern Research
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Bristol-Myers Squibb
Active site-directed plasmin inhibitors: Extension on the P2 residue.
Kobe Gakuin University
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.
Aurigene Discovery Technologies
Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors.
Heidelberg University
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.
Queensland University of Technology
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.
Southeast University
Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.
Tokyo University of Pharmacy and Life Sciences
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Rempex Pharmaceuticals
Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.
Bristol-Myers Squibb R & D
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Bristol-Myers Squibb
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
Bristol-Myers Squibb
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.
Astellas Pharma
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.
Astellas Pharma
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Bristol-Myers Squibb
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.
Chinese Academy of Sciences
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.
Berlex Biosciences
Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.
Astrazeneca
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.
Johnson & Johnson Pharmaceutical Research & Development
GRID/CPCA: a new computational tool to design selective ligands.
Boehringer Ingelheim Pharma
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.
Corvas International
Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.
Peking University
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease.
Irbm
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.
The University of Arizona
Small molecules targeting ?-secretase and their potential biological applications.
Shenyang Pharmaceutical University
Discovery of potent benzoxaborole inhibitors against SARS-CoV-2 main and dengue virus proteases.
Heidelberg University
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Kalvista Pharmaceuticals
Potent Cyclic Peptide Inhibitors of FXIIa Discovered by mRNA Display with Genetic Code Reprogramming.
The University of Sydney
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Eli Lilly
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE).
TBA
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Merck Research Laboratories
Factor XII/XIIa inhibitors: Their discovery, development, and potential indications.
University of Namur
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.
National Cancer Institute-Frederick
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.
Axys Pharmaceuticals
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Merck
A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays.
Heidelberg University
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.
Qpex Biopharma
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.
Dupont Pharmaceuticals
The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.
Roche Discover Welwyn
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.
The University of Queensland
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.
Philipps University Marburg
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.
University of Wollongong
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.
China Pharmaceutical University
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
Biotech Research Institute
Potential Anticancer Agents Characterized from Selected Tropical Plants.
The Ohio State University
Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors.
Heidelberg University
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.
The University of Queensland
3-Acyltetramic acids as a novel class of inhibitors for human kallikreins 5 and 7.
Universidade Federal Fluminense
Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.
The University of Queensland
Protease inhibitors from Microcystis aeruginosa bloom material collected from the Dalton Reservoir, Israel.
Tel-Aviv University
Aeruginosins from a Microcystis sp. bloom material collected in Varanasi, India.
Tel-Aviv University
Metabolites from Microcystis aeruginosa bloom material collected at a water reservoir near Kibbutz Hafetz Haim, Israel.
Tel-Aviv University
HCV-NS3/4A protease inhibitory iridoid glucosides and dimeric foliamenthoic acid derivatives from Anarrhinum orientale.
Cairo University
Effects of flavonoids isolated from scutellariae radix on fibrinolytic system induced by trypsin in human umbilical vein endothelial cells.
Ehime University
Synthesis of fluorescent-labeled aeruginosin derivatives for high-throughput fluorescence correlation spectroscopy assays.
Graduate School of Science and Engineering
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.
University of Nottingham
Structure-based drug design of 1,3,6-trisubstituted 1,4-diazepan-7-ones as selective human kallikrein 7 inhibitors.
Asubio Pharma
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity.
German Cancer Research Center (Dkfz)
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
University of Wollongong
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.
Hefei University of Technology
Discovery and structure-activity relationship study of 1,3,6-trisubstituted 1,4-diazepane-7-ones as novel human kallikrein 7 inhibitors.
Asubio Pharma
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1.
The University of Queensland