71 articles for thisTarget
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PMID
Data
Article Title
Organization
Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.
Bristol-Myers Squibb
Discovery of a new isomannide-based peptidomimetic synthetized by Ugi multicomponent reaction as human tissue kallikrein 1 inhibitor.
Universidade Federal Fluminense
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.
Bristol-Myers Squibb R & D
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.
Bristol-Myers Squibb Research & Development
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
The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins.
Campus
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Bristol-Myers Squibb
Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.
Universidade De Lisboa
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
Kallikrein protease activated receptor (PAR) axis: an attractive target for drug development.
University of Naples Federico II
Human kallikrein 6 inhibitors with a para-amidobenzylanmine P1 group identified through virtual screening.
Sanofi Pharmaceuticals
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.
Klinikum Der Friedrich-Schiller-Universit£T Jena
Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.
Thrombosis Research Institute
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.
Novartis Horsham Research Centre
Synthesis of potent and selective inhibitors of human plasma kallikrein.
The Procter & Gamble
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.
Universit£T Bielefeld
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors
TBA
Discovery and development of plasma kallikrein inhibitors for multiple diseases.
Hefei University of Technology
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
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Abbott Laboratories
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.
Millennium Pharmaceuticals
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.
Millennium Pharmaceuticals
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Millennium Pharmaceuticals
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.
Millennium Pharmaceuticals
Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation.
Sorbonne Universit£
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.
Millennium Pharmaceuticals
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.
Millennium Pharmaceuticals
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Kallikrein 5 inhibitors identified through structure based drug design in search for a treatment for Netherton Syndrome.
Glaxosmithkline R&D
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Glaxosmithkline
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.
Glaxosmithkline R&D
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.
Molecumetics
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.
Aarhus University
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.
Thrombosis Research Institute
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
Neutral macrocyclic factor VIIa inhibitors.
Bristol-Myers Squibb Research and Development
4-AMINO-3-(4-PHENOXYPHENYL)-1,3-DIHYDRO-2H-IMIDAZO[4,5-C]PYRIDIN-2-ONE DERIVATIVES AND SALTS THEREOF
Genzyme
OXA- IBOGAINE INSPIRED ANALOGUES FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
Columbia University
HALOALKYLPYRIDYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR
Huyabio International
Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
Vertex Pharmaceuticals
Monocyclic thieno, pyrido, and pyrrolo pyrimidine compounds and methods of use and manufacture of same
Duquesne University of The Holy Spirit
Deciphering the binding of caveolin-1 to client protein endothelial nitric-oxide synthase (eNOS): scaffolding subdomain identification, interaction modeling, and biological significance.
St. Paul'S Hospital'S Centre of Heart and Lung Innovation
A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer.
Universität Duisburg-Essen
Heterocyclic group contained amino-methanol derivative, and salt, synthetic method and use thereof
Beijing Foreland Biopharma
Specialization among iron-sulfur cluster helicases to resolve G-quadruplex DNA structures that threaten genomic stability.
National Institutes of Health, National Institutes of Health Biomedical Research Center
Synthesis and Biological Evaluation of 3-thiazolocoumarinyl Schiff-base Derivatives as Cholinesterase Inhibitors.
Comsats Institute of Information Technology