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203 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.EBI
Bristol-Myers Squibb
Synthesis of a cyanopeptide-analogue with trypsin activating properties.EBI
Ernst-Moritz-Arndt-University
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.EBI
Global Blood Therapeutics
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.EBI
Bristol-Myers Squibb R & D
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.EBI
Bristol-Myers Squibb R & D
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.EBI
Bristol-Myers Squibb
Active site-directed plasmin inhibitors: Extension on the P2 residue.EBI
Kobe Gakuin University
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.EBI
Aurigene Discovery Technologies
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.EBI
Queensland University Of Technology
Pyridine and pyridinone-based factor XIa inhibitors.EBI
Bristol-Myers Squibb
Inhibitors of melanogenesis in B16 melanoma 4A5 cells from flower buds of Lawsonia inermis (Henna).EBI
Kyoto Pharmaceutical University
Novel type of plasmin inhibitors: providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine.EBI
Hiroshima International University
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.EBI
Rempex Pharmaceuticals
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI
Bristol-Myers Squibb
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.EBI
Astrazeneca
Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy.EBI
Aurigene Discovery Technologies
Inhibition of four human serine proteases by substituted benzamidines.EBI
TBA
Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.EBI
TBA
Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin.EBI
Hiroshima International University
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.EBI
Bristol-Myers Squibb
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.EBI
Sanofi-Aventis R&D
Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.EBI
Emory University
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.EBI
Lg Life Sciences
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.EBI
Ecole Polytechnique F�D�Rale De Lausanne Epfl
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.EBI
Astrazeneca
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI
Philipps University Marburg
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.EBI
Celera Genomics
Development of activity-based probes for trypsin-family serine proteases.EBI
Celera Genomics
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.EBI
Aarhus University
Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.EBI
Zydus Research Centre
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.EBI
Hokkaido University
A new strategy for the development of highly potent and selective plasmin inhibitors.EBI
Philipps University Marburg
2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.EBI
University Of Louisville
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.EBI
Takeda Pharmaceutical
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI
University Of Florida
Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.EBI
Chiba University
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI
Johnson & Johnson Pharmaceutical Research & Development
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.EBI
Bristol-Myers Squibb Research And Development
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.EBI
University Of Antwerp
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.EBI
Bristol-Myers Squibb
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.EBI
Abbott
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.EBI
Brown University
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.EBI
Central Pharmaceutical Research Institute
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.EBI
Central Pharmaceutical Research Institute
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).EBI
Pharmaceutical Research Institute
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.EBI
Lg Life Sciences
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.EBI
Dupont Pharmaceuticals
Protease inhibitors: current status and future prospects.EBI
University Of Queensland
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.EBI
Novartis Horsham Research Centre
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI
Rh£Ne-Poulenc Rorer
Tetrahydro-isoquinoline-based factor Xa inhibitors.EBI
Boehringer Mannheim
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.EBI
Merck Research Laboratories
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.EBI
Merck Research Laboratories
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.EBI
Klinikum Der Friedrich-Schiller-Universit£T Jena
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.EBI
Abbott Laboratories
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.EBI
Universit£
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.EBI
Novartis Horsham Research Centre
 
Design and synthesis of conformationally constrained arginal thrombin inhibitorsEBI
TBA
 
DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORSEBI
TBA
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).EBI
University Of Antwerp
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI
Bristol-Myers Squibb
Identification of novel plasmin inhibitors possessing nitrile moiety as warhead.EBI
Hiroshima International University
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.EBI
Philipps University Marburg
New furin inhibitors based on weakly basic amidinohydrazones.EBI
Philipps University Marburg
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.EBI
F. Hoffmann-La Roche
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.EBI
University Of Basel
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.EBI
Takeda Pharmaceutical
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.EBI
Johnson & Johnson Pharmaceutical Research And Development
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.EBI
Philipps University Marburg
Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).EBI
Berlex Biosciences
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI
Bristol-Myers Squibb
 
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moietyEBI
TBA
 
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI
TBA
 
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogatesEBI
TBA
 
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitorsEBI
TBA
 
(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitorsEBI
TBA
 
Characterization of LY806303 as a potent and selective inhibitor of thrombinEBI
TBA
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.EBI
Millennium Pharmaceuticals
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.EBI
Millennium Pharmaceuticals
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.EBI
The Medicines Company (Leipzig)
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.EBI
Daiichi Sankyo
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.EBI
Curacyte Discovery
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.EBI
University Of ZüRich
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.EBI
Bristol-Myers Squibb
Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI
Glaxosmithkline
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.EBI
University Of Antwerp
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.EBI
Celera Genomics
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.EBI
Mochida Pharmaceutical
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.EBI
Johnson & Johnson Pharmaceutical Research And Development
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
9-hydroxyazafluorenes and their use in thrombin inhibitors.EBI
Merck Research Laboratories
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.EBI
Abbott Laboratories
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.EBI
Eli Lilly
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.EBI
Pfizer
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.EBI
Abbott Laboratories
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.EBI
University Of Antwerp
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.EBI
Millennium Pharmaceuticals
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.EBI
Abbott Laboratories
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.EBI
The Bristol-Myers Squibb Pharmaceutical Research Institute
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.EBI
Boehringer Ingelheim Pharma
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI
Boehringer Ingelheim Pharma
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI
3-Dimensional Pharmaceuticals
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI
Celera
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI
Celera
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.EBI
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.EBI
Millennium Pharmaceuticals
Structure-based design of novel potent nonpeptide thrombin inhibitors.EBI
Boehringer Ingelheim Pharma
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.EBI
Aventis Pharmaceuticals
4-amidinobenzylamine-based inhibitors of urokinase.EBI
Universitat Jena
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.EBI
Pfizer
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.EBI
Pfizer
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.EBI
Cor Therapeutics
Optimization of a screening lead for factor VIIa/TF.EBI
Axys Pharmaceuticals
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.EBI
Axys Pharmaceuticals
Development of potent and selective factor Xa inhibitors.EBI
Axys Pharmaceuticals
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI
Shionogi
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.EBI
Axys Pharmaceuticals
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.EBI
3-Dimensional Pharmaceuticals
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.EBI
Novartis Institutes For Biomedical Research
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.EBI
Bristol Myers Squibb
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.EBI
Qpex Biopharma
Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.EBI
Institute Of Molecular And Cell Biology
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI
Shionogi
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.EBI
Pfizer
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.EBI
Axys Pharmaceuticals
Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.EBI
Axys Pharmaceuticals
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.EBI
Corvas International
Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and HT29 cell lines.EBI
Kobe Gakuin University
Nonbenzamidine compounds as selective factor Xa inhibitors.EBI
Aventis Pharmaceuticals
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.EBI
Novartis Horsham Research Centre
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.EBI
The University Of Queensland
Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.EBI
Corvas International
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.EBI
Astrazeneca
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.EBI
Philipps University Marburg
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI
Corvas International
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.EBI
Chinese Academy Of Sciences
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI
Rhone-Poulenc Rorer
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.EBI
University Of Wollongong
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates.EBI
Corvas International
3-Amidinophenylalanine-based inhibitors of urokinase.EBI
UniversitäT Jena
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI
RhôNe-Poulenc Rorer
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.EBI
Brown University
Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI
Corvas International
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.EBI
Bristol-Myers Squibb
4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.EBI
Brown University
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.EBI
Novartis Horsham Research Centre
Thrombin inhibitors based on a propargylglycine template.EBI
Biotech Research Institute
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.EBI
Corvas International
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.EBI
The University Of Queensland
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI
Dupont Pharmaceuticals
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI
Corvas International
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.EBI
3-Dimensional Pharmaceuticals
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.EBI
Bristol-Myers Squibb
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.EBI
Philipps University Marburg
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI
Biotech Research Institute
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of benzamidine-type inhibitors of factor Xa.EBI
Institut FüR Biochemie
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.EBI
Merck Research Laboratories
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.EBI
The University Of Queensland
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.EBI
Merck Research Laboratories
Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity.EBI
Hiroshima International University
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.EBI
University Of Antwerp (Ua)
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.EBI
Aarhus University
Highly selective tripeptide thrombin inhibitors.EBI
Eli Lilly
Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI
Thrombosis Research Institute
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI
Eli Lilly
Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis.EBI
The University Of Tokyo
Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica.EBI
The University Of Tokyo
Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.EBI
TBA
Isolation and structure determination of nostocyclopeptides A1 and A2 from the terrestrial cyanobacterium Nostoc sp. ATCC53789.EBI
University Of Hawaii At Manoa
Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.EBI
Abdulaziz University For Health Sciences
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.EBI
University Of Nottingham
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.EBI
Bristol-Myers Squibb
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.EBI
University Of Wollongong
Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold.EBI
The University Of Queensland
Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.EBI
Virginia Commonwealth University
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.EBI
Bicycle Therapeutics
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).EBI
Bristol-Myers Squibb
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.EBI
University Of Illinois
Neutral macrocyclic factor VIIa inhibitors.EBI
Bristol-Myers Squibb Research And Development
 
Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazolesBDB
Hacettepe University
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB
Uppsala University
Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors.BDB
Durham University