186 articles for thisTarget
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Article Title
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Guanidinophenyl-substituted enol lactones as selective, mechanism-based inhibitors of trypsin-like serine proteases.
University of Illinois
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
Nostosins, Trypsin Inhibitors Isolated from the Terrestrial Cyanobacterium Nostoc sp. Strain FSN.
University of Helsinki
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
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.
Berlex Biosciences
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.
Berlex Biosciences
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.
Lg Life Sciences
GRID/CPCA: a new computational tool to design selective ligands.
Boehringer Ingelheim Pharma
Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.
R. W. Johnson Pharmaceutical Research Institute
Design and synthesis of potent and highly selective thrombin inhibitors.
F. Hoffmann-La Roche
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.
University of Arkansas
New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue.
Cnrs-Cercoa
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.
Abbott Laboratories
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
The Bristol-Myers Squibb Pharmaceutical Research Institute
D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.
Basf
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.
Life Science R & D, Lgci
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.
Corvas International
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.
Medical University of South Carolina
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors
TBA
Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor
TBA
Kinetic characterization of a peptide inhibitor of trypsin isolated from a synthetic peptide combinatorial library
TBA
Inhibitory activity of unsaturated fatty acids and anacardic acids toward soluble tissue factor-factor VIIa complex.
Searle Discovery Research
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 γ-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
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Abbott Laboratories
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
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.
University of Ljubljana
Synthesis of 2-guanidinyl pyridines and their trypsin inhibition and docking.
University College Dublin
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Merck Research Laboratories
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
A mechanism-based probe for gp120-Hydrolyzing antibodies.
University of Texas-Houston Medical School
Factor XII/XIIa inhibitors: Their discovery, development, and potential indications.
University of Namur
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.
Protherics Molecular Design
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-β-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
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
Shionogi
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.
The University of Queensland
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.
Berlex Biosciences
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.
Philipps University Marburg
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.
Kyoto Pharmaceutical University
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.
Berlex Biosciences
Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.
3-Dimensional Pharmaceuticals
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.
University of Wollongong
Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.
3-Dimensional Pharmaceuticals
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.
Washington University
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
Biotech Research Institute
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.
Berlex Biosciences
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.
Molecumetics
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.
China Pharmaceutical University
Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.
The University of Queensland
Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.
Nv Organon Scientific Development Group
N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.
Nippon Steel
Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.
Institut FüR Biochemie
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.
The University of Queensland
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
Dupont Pharmaceuticals
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
Biotech Research Institute
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.
Berlex Biosciences
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.
Biotech Research Institute
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
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.
Novartis Pharma
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
Berlex Biosciences
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.
Berlex Biosciences
Protein-Induced Change in Ligand Protonation during Trypsin and Thrombin Binding: Hint on Differences in Selectivity Determinants of Both Proteins?
Philipps-University Marburg
Assessment of solvation effects on calculated binding affinity differences: trypsin inhibition by flavonoids as a model system for congeneric series.
Universidad De Alcalá
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Merck Research Laboratories
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
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.
Aarhus University
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
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.
Thrombosis Research Institute
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.
Eli Lilly
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
Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.
TBA
Three-dimensional quantitative structure-activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices analysis to elucidate selectivity differences of inhibitors binding to trypsin, thrombin, and factor Xa.
University of Marburg
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
Cyclotides, a versatile ultrastable micro-protein scaffold for biotechnological applications.
University of Southern California
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
Jizanpeptins, Cyanobacterial Protease Inhibitors from a Symploca sp. Cyanobacterium Collected in the Red Sea.
Oregon State University
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.
Merck Sharp and Dohme Research Laboratories
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.
University of Illinois
Spiro-sulfonamide derivatives as inhibitors of myeloid cell leukemia-1 (MCL-1) protein
Prelude Therapeutics
Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
Janssen Pharmaceutica
Compounds inhibiting eukaryotic elongation factor 2 kinase activity
Longevica Pharmaceuticals
Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors
Vtv Therapeutics
5-aminopyrazole-4-carboxamide inhibitors of CDPK1 from T. gondii and C. parvum
University of Washington Through Its Center For Commercialization
Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists
Rugen Holdings (Cayman)
3-oxo-2,3-dihydro-1H-isoindole-4-carboxamides with selective PARP-1 inhibition
Nerviano Medical Sciences
Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2.
Wyeth Research
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.
University of Antwerp
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1.
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines.
Wyeth-Ayerst Research
Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors.
Wyeth Research
Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.
Gilead Sciences
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.
Yamanouchi Pharmaceutical
Systematic structure-based design and stereoselective synthesis of novel multisubstituted cyclopentane derivatives with potent antiinfluenza activity.
Biocryst Pharmaceuticals
Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.
Sugen
Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase.
Biocryst Pharmaceuticals
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design.
Biocryst Pharmaceuticals
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Glaxosmithkline
Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.
Astrazeneca