161 articles for thisTarget
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Article Title
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Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.
Bristol-Myers Squibb
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.
Global Blood Therapeutics
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.
Bristol-Myers Squibb R & D
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Bristol-Myers Squibb R & D
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.
Bristol-Myers Squibb Research & Development
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Bristol-Myers Squibb
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.
Institute For Infection Research
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
A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.
Virginia Commonwealth University
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
Allosteric inhibition of human factor XIa: discovery of monosulfated benzofurans as a class of promising inhibitors.
Virginia Commonwealth University
Inhibitors of Factor XIa and Plasma Kallikrein May Treat Thromboembolic Disorders and Many Diabetes Complications.
Therachem Research Medilab (India)
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.
Astrazeneca
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.
Bristol-Myers Squibb R & D
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.
Bristol-Myers Squibb Research & Development
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Bristol-Myers Squibb
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.
Ecole Polytechnique F�D�Rale De Lausanne Epfl
Discovery of allosteric modulators of factor XIa by targeting hydrophobic domains adjacent to its heparin-binding site.
Virginia Commonwealth University
Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.
Virginia Commonwealth University
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Celera Genomics
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.
Virginia Commonwealth University
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bristol-Myers Squibb Research and Development
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
Bristol-Myers Squibb
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.
Daiichi Asubio Medical Research Laboratories
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.
University of Montreal
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Bristol-Myers Squibb
Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.
Université
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
F. Hoffmann-La Roche
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.
University of Basel
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.
Chugai Pharmaceutical
Clavatadine A, a natural product with selective recognition and irreversible inhibition of factor XIa.
Griffith University
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders.
Bayer
Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Verseon
Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives.
Hefei University of Technology
Designing Smaller, Synthetic, Functional Mimetics of Sulfated Glycosaminoglycans as Allosteric Modulators of Coagulation Factors.
Virginia Commonwealth University
Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.
University of Nottingham
Studies on fragment-based design of allosteric inhibitors of human factor XIa.
Virginia Commonwealth University
Discovery and development of plasma kallikrein inhibitors for multiple diseases.
Hefei University of Technology
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.
Daiichi Asubio Medical Research Laboratories
Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Janssen Research & Development
Factor XI Activation Inhibitors for Treating Thromboses, Embolism, Hypercoagulability, or Fibrotic Changes.
Smith, Gambrell & Russell
Development of Selective FXIa Inhibitors Based on Cyclic Peptides and Their Application for Safe Anticoagulation.
Ecole Polytechnique F�D�Rale De Lausanne (Epfl)
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
Targeting the S2 Subsite Enables the Structure-Based Discovery of Novel Highly Selective Factor XIa Inhibitors.
Hefei University of Technology
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Factor XI Activation Inhibitors for Treating Thrombosis, Embolisms, Hypercoagulability, and Fibrotic Changes.
Smith, Gambrell & Russell
Factor XI Activation Inhibitors for Treating Thrombosis, Embolisms, Hypercoagulability, and Fibrotic Changes.
Smith, Gambrell & Russell
Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment.
Shenyang Pharmaceutical University
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Novartis Institutes For Biomedical Research
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Merck
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Novartis Institutes For Biomedical Research
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.
Bristol-Myers Squibb
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.
The University of Queensland
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.
Astrazeneca
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.
Philipps University Marburg
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.
Chinese Academy of Sciences
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 Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Novartis Institutes For Biomedical Research
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.
The University of Queensland
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.
Philipps University Marburg
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.
Aarhus University
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.
University of Nottingham
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
University of Wollongong
Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.
Bristol-Myers Squibb
Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.
Virginia Commonwealth University
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Bicycle Therapeutics
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Bristol-Myers Squibb
SHP2-Targeting Small Molecules For Use As Anti-Cancer Agents
West Virginia University
4-AMINO-3-(4-PHENOXYPHENYL)-1,3-DIHYDRO-2H-IMIDAZO[4,5-C]PYRIDIN-2-ONE DERIVATIVES AND SALTS THEREOF
Genzyme
MODIFIED IMIDAZOPYRIDINES AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
Merck Sharp & Dohme
OXA- IBOGAINE INSPIRED ANALOGUES FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
Columbia University
HALOALKYLPYRIDYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR
Huyabio International
Dopamine D3 receptor selective antagonists/partial agonists and uses thereof
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
Vertex Pharmaceuticals
Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
Bristol-Myers Squibb
2-quinolone derived inhibitors of BCL6
The Institute of Cancer Research: Royal Cancer Hospital
3-substituted 5-amino-6H-thiazolo[4,5-D]pyrimidine-2, 7-dione compounds for the treatment and prophylaxis of virus infection
Hoffmann-La Roche
4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
Boehringer Ingelheim International
D-amino acid oxidase inhibitors and therapeutic uses thereof
SyneuRx International (Taiwan)
[4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof
Santen Pharmaceutical
In vitro effects of cinnamic acid derivatives on protein tyrosine phosphatase 1B.
Chulalongkorn University
Structural basis for the recognition of peptide RJPXD33 by acyltransferases in lipid A biosynthesis.
University of Michigan
A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer.
Universität Duisburg-Essen
Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitors
Taibah University
Heterocyclic group contained amino-methanol derivative, and salt, synthetic method and use thereof
Beijing Foreland Biopharma
Inhibition of Pax2 Transcription Activation with a Small Molecule that Targets the DNA Binding Domain.
University of Michigan
Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption.
Western University
Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches.
Sanofi Oncology
The chlorite dismutase (HemQ) from Staphylococcus aureus has a redox-sensitive heme and is associated with the small colony variant phenotype.
University of Notre Dame
4-alkoxy-N-(2-hydroxycarbamoyl-2-piperidinyl-ethyl)-benzamide compounds as selective TACE-inhibitors for the treatment of inflammatory diseases
Galderma Research & Development
A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition.
Jawaharlal Nehru Centre For Advanced Scientific Research
5-fluoro-3-phenyl-2-[1-(9h-purin-6-ylamino)propyl]-3h-quinazolin-4-one as an inhibitor of human phosphatidylinositol 3-kinase delta
Icos
Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
Boehringer Ingelheim International
Substituted pyrido[3,2-E][1,2,4]-triazolo[4,3-A]pyrazines for the treatment of central nervous system disorders
Boehringer Ingelheim International
Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents
Boehringer Ingelheim International
[3H]-Mesulergine labels 5-HT7 sites in rat brain and guinea-pig ileum but not rat jejunum.
Monash University
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Smithkline Beecham Pharmaceuticals
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.
National Institute of Mental Health
Structure-based dissection of the natural product cyclopentapeptide chitinase inhibitor argifin.
University of Dundee
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines.
Wyeth-Ayerst Research