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206 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28085275 53 Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.EBI Bristol-Myers Squibb
10782685 9 Synthesis of a cyanopeptide-analogue with trypsin activating properties.EBI Ernst-Moritz-Arndt-University
28197309 40 Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.EBI Global Blood Therapeutics
27994741 48 Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.EBI Bristol-Myers Squibb R & D
27455395 66 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
27073051 71 Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.EBI Bristol-Myers Squibb
26732532 69 Active site-directed plasmin inhibitors: Extension on the P2 residue.EBI Kobe Gakuin University
26421993 44 Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.EBI Aurigene Discovery Technologies
26393374 34 Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.EBI Queensland University of Technology
25592713 37 Pyridine and pyridinone-based factor XIa inhibitors.EBI Bristol-Myers Squibb
25987378 2 Inhibitors of melanogenesis in B16 melanoma 4A5 cells from flower buds of Lawsonia inermis (Henna).EBI Kyoto Pharmaceutical University
25921265 21 Novel type of plasmin inhibitors: providing insight into P4 moiety and alternative scaffold to pyrrolopyrimidine.EBI Hiroshima International University
25782055 9 Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.EBI Rempex Pharmaceuticals
25728130 79 Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI Bristol-Myers Squibb
24900876 56 Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.EBI Astrazeneca
152812 69 Inhibition of four human serine proteases by substituted benzamidines.EBI TBA
660589 3 Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.EBI TBA
24613052 69 Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin.EBI Hiroshima International University
24405333 69 Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.EBI Bristol-Myers Squibb
24175584 35 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
24135727 7 Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.EBI Emory University
23899618 9 Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.EBI Lg Life Sciences
23586812 38 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
23521080 6 Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.EBI Astrazeneca
23294255 114 Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI Philipps University Marburg
16644215 52 Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.EBI Celera Genomics
16554154 9 Development of activity-based probes for trypsin-family serine proteases.EBI Celera Genomics
22882079 26 Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.EBI Aarhus University
23124211 22 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
22950366 6 Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.EBI Hokkaido University
22276953 63 A new strategy for the development of highly potent and selective plasmin inhibitors.EBI Philipps University Marburg
22366654 33 2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.EBI University of Louisville
19861238 14 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
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
15787457 3 Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.EBI Chiba University
18164204 24 Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.EBI Takeda Pharmaceutical
18053726 364 Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI Johnson & Johnson Pharmaceutical Research & Development
18077174 31 Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.EBI Takeda Pharmaceutical
18054227 45 Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.EBI Bristol-Myers Squibb Research and Development
18052026 97 Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.EBI University of Antwerp
17588746 103 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
16517159 45 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.EBI Abbott
16250649 10 Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.EBI Brown University
15887966 58 Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.EBI Central Pharmaceutical Research Institute
15582437 2 Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors.EBI Central Pharmaceutical Research Institute
14640539 112 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
12904065 30 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
11170646 106 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
10669559 180 Protease inhibitors: current status and future prospects.EBI University of Queensland
10579821 51 Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.EBI Novartis Horsham Research Centre
10479288 141 Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI Rh£Ne-Poulenc Rorer
9836616 92 Tetrahydro-isoquinoline-based factor Xa inhibitors.EBI Boehringer Mannheim
9083470 9 Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.EBI Merck Research Laboratories
9357536 47 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
9301673 234 Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.EBI Klinikum Der Friedrich-Schiller-Universit£T Jena
2231595 96 Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.EBI Abbott Laboratories
12270173 23 Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.EBI Universit£
10915051 43 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
 22 Design and synthesis of conformationally constrained arginal thrombin inhibitorsEBI TBA
 48 DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORSEBI TBA
22285569 107 Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).EBI University of Antwerp
22041058 44 Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI Bristol-Myers Squibb
21944858 12 Identification of novel plasmin inhibitors possessing nitrile moiety as warhead.EBI Hiroshima International University
21741839 83 Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.EBI Philipps University Marburg
21168329 47 New furin inhibitors based on weakly basic amidinohydrazones.EBI Philipps University Marburg
20650636 118 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
20405925 5 Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.EBI University of Basel
20355714 26 Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.EBI Takeda Pharmaceutical
20102150 35 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
20038105 50 Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.EBI Philipps University Marburg
19703768 63 Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).EBI Berlex Biosciences
19541481 57 Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI Bristol-Myers Squibb
 15 Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moietyEBI TBA
 37 Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI TBA
 25 Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogatesEBI TBA
 78 Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitorsEBI TBA
 61 (N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitorsEBI TBA
 13 Characterization of LY806303 as a potent and selective inhibitor of thrombinEBI TBA
19297158 30 Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.EBI Millennium Pharmaceuticals
19297154 88 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
19250826 100 Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.EBI The Medicines Company (Leipzig)
19128974 28 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
19036586 128 Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.EBI Curacyte Discovery
18507371 24 Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.EBI Takeda Pharmaceutical
17935298 3 Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.EBI University of ZüRich
17643988 92 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
17420122 18 Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI Glaxosmithkline
16970403 74 Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.EBI University of Antwerp
16725321 13 Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.EBI Celera Genomics
16540315 23 Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.EBI Mochida Pharmaceutical
16460935 39 A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.EBI Johnson & Johnson Pharmaceutical Research and Development
16213711 37 Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15801822 28 9-hydroxyazafluorenes and their use in thrombin inhibitors.EBI Merck Research Laboratories
15582418 103 Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.EBI Abbott Laboratories
15341970 59 P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.EBI Eli Lilly
15149680 58 Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.EBI Pfizer
15149645 92 Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.EBI Abbott Laboratories
15115382 16 Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.EBI University of Antwerp
15013007 319 Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.EBI Millennium Pharmaceuticals
14711304 117 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
14698147 60 Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
12824021 39 Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.EBI Boehringer Ingelheim Pharma
12824020 31 Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI Boehringer Ingelheim Pharma
12668020 29 Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals
12639567 135 Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI Millennium Pharmaceuticals
12372529 21 Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12113833 183 4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI Celera
12113832 120 2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI Celera
12039584 59 Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.EBI Millennium Pharmaceuticals
12039583 140 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
11960487 30 Structure-based design of novel potent nonpeptide thrombin inhibitors.EBI Boehringer Ingelheim Pharma
11958994 31 Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.EBI Aventis Pharmaceuticals
11844691 107 4-amidinobenzylamine-based inhibitors of urokinase.EBI Universitat Jena
11755350 31 Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.EBI Pfizer
11755349 24 Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.EBI Pfizer
11677132 65 Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.EBI Cor Therapeutics
11527709 19 Optimization of a screening lead for factor VIIa/TF.EBI Axys Pharmaceuticals
11495587 198 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
11459634 94 Development of potent and selective factor Xa inhibitors.EBI Axys Pharmaceuticals
11425539 23 Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI Shionogi
11425524 62 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
11378359 57 Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.EBI 3-Dimensional Pharmaceuticals
32551603 185 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
32456431 24 Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.EBI Bristol Myers Squibb
32150407 27 Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.EBI Qpex Biopharma
11206478 18 Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.EBI Institute of Molecular and Cell Biology
11078187 36 Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI Shionogi
11063603 53 Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.EBI Pfizer
11055356 236 Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.EBI Axys Pharmaceuticals
11055355 72 Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.EBI Axys Pharmaceuticals
11055344 37 Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.EBI Corvas International
11012033 8 Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and HT29 cell lines.EBI Kobe Gakuin University
10937736 35 Nonbenzamidine compounds as selective factor Xa inhibitors.EBI Aventis Pharmaceuticals
10915052 20 The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors.EBI Novartis Horsham Research Centre
27434175 54 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
10853674 32 Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.EBI Corvas International
27347787 32 Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.EBI Astrazeneca
27280436 304 Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.EBI Philipps University Marburg
10782677 73 Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI Corvas International
30707839 63 Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.EBI Chinese Academy of Sciences
10698439 68 Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI Rhone-Poulenc Rorer
31679971 44 6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.EBI University of Wollongong
10617091 73 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
10560742 85 3-Amidinophenylalanine-based inhibitors of urokinase.EBI UniversitäT Jena
10509929 116 Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI RhôNe-Poulenc Rorer
10508448 11 Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.EBI Brown University
10498211 42 Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI Corvas International
31445854 43 Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.EBI Bristol-Myers Squibb
10425106 12 4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.EBI Brown University
10328293 23 The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.EBI Novartis Horsham Research Centre
10230630 36 Thrombin inhibitors based on a propargylglycine template.EBI Biotech Research Institute
10206557 36 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
30520638 54 Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.EBI The University of Queensland
9873692 54 Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI Dupont Pharmaceuticals
9873569 16 Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI Corvas International
9873397 37 In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals
31833761 32 Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.EBI Bristol-Myers Squibb
31658420 98 Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.EBI Philipps University Marburg
9871573 15 Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI Biotech Research Institute
9822554 14 1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
9784099 84 Design of benzamidine-type inhibitors of factor Xa.EBI Institut FüR Biochemie
9703466 35 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
30613336 32 Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.EBI The University of Queensland
9171866 12 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
27009905 22 Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity.EBI Hiroshima International University
26575094 60 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)
26536069 89 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
8426361 111 Highly selective tripeptide thrombin inhibitors.EBI Eli Lilly
8423602 15 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
8035417 23 Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
7739010 118 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI Thrombosis Research Institute
7473571 90 Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI Eli Lilly
9722497 2 Aeruginosin 103-A, a thrombin inhibitor from the cyanobacterium Microcystis viridis.EBI The University of Tokyo
9644086 1 Dehydroradiosumin, a trypsin inhibitor from the cyanobacterium Anabaena cylindrica.EBI The University of Tokyo
6219223 94 Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.EBI TBA
11170666 6 Isolation and structure determination of nostocyclopeptides A1 and A2 from the terrestrial cyanobacterium Nostoc sp. ATCC53789.EBI University of Hawaii At Manoa
30201291 27 Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.EBI Abdulaziz University For Health Sciences
29072911 16 Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.EBI University of Nottingham
29501396 59 Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.EBI Bristol-Myers Squibb
30130401 71 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
28045523 35 Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold.EBI The University of Queensland
27976897 39 Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.EBI Virginia Commonwealth University
29517911 87 Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.EBI Bicycle Therapeutics
29077405 63 Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).EBI Bristol-Myers Squibb
1447734 29 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
28460818 29 Neutral macrocyclic factor VIIa inhibitors.EBI Bristol-Myers Squibb Research and Development
 18 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
9802391 31 The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB Uppsala University
24058293 12 Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors.BDB Durham University