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499 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27166573 24 Molecular design, synthesis and anticoagulant activity evaluation of fluorinated dabigatran analogues.EBI Shanghai Institute of Technology
26985294 114 Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.EBI Southern Research
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 Company
26704266 80 Novel phenylalanine derived diamides as Factor XIa inhibitors.EBI Bristol-Myers Squibb Company
26421993 44 Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.EBI Aurigene Discovery Technologies Limited
26200936 39 Applications of Fluorine in Medicinal Chemistry.EBI Bristol-Myers Squibb Research and Development
26537784 4 Design, synthesis and antithrombotic evaluation of novel dabigatran etexilate analogs, a new series of non-peptides thrombin inhibitors.EBI China Pharmaceutical University
26367391 6 Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors.EBI Heidelberg University
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
26288158 13 Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein-Ligand Complexes.EBI University of Michigan
26114810 8 Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.EBI Southeast University
26270568 18 Fragment Binding Can Be Either More Enthalpy-Driven or Entropy-Driven: Crystal Structures and Residual Hydration Patterns Suggest Why.EBI Philipps-University Marburg
26122211 3 Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.EBI Tokyo University of Pharmacy and Life Sciences
26151189 56 Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.EBI TBA
26005539 23 Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.EBI Bristol-Myers Squibb
25990761 66 Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.EBI Institute for Infection Research
25782055 9 Discovery of a Cyclic Boronic Acid▀-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.EBI Rempex Pharmaceuticals, Inc.
25912673 48 Binding cooperativity between a ligand carbonyl group and a hydrophobic side chain can be enhanced by additional H-bonds in a distance dependent manner: A case study with thrombin inhibitors.EBI The State University of New York
25874337 23 Design, synthesis and structural exploration of novel fluorinated dabigatran derivatives as direct thrombin inhibitors.EBI Shanghai Institute of Technology
25839438 19 Identification of anthranilamide derivatives as potential factor Xa inhibitors: drug design, synthesis and biological evaluation.EBI China Pharmaceutical University
25881820 62 Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.EBI Bristol-Myers Squibb R&D
25728130 79 Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI Bristol-Myers Squibb Company
25650311 76 Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.EBI Chang Gung University
25559742 6 Design, synthesis and evaluation of isoxazolo[5,4-d]pyrimidin-4(5H)-one derivatives as antithrombotic agents.EBI Southeast University
24951330 25 Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.EBI Bristol-Myers Squibb Company
25523211 18 Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.EBI Astellas Pharma Inc.
25453807 13 A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.EBI Virginia Commonwealth University
25438755 9 Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.EBI Astellas Pharma Inc.
25405503 109 Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.EBI Bristol-Myers Squibb
25268757 16 How a▀-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties.EBI Consiglio Nazionale delle Ricerche
25179681 81 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.EBI Chinese Academy of Sciences
24794746 168 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 Limited
1271404 55 Novel bis(benzamidino) compounds with an aromatic central link. Inhibitors of thrombin, pancreatic kallikrein, trypsin, and complement.EBI TBA
152812 69 Inhibition of four human serine proteases by substituted benzamidines.EBI TBA
722718 56 Structure-activity relationships for the inhibition of acrosin by benzamidine derivatives.EBI TBA
671460 122 Diarylamidine derivatives with one or both of the aryl moieties consisting of an indole or indole-like ring. Inhibitors of arginine-specific esteroproteases.EBI TBA
660589 3 Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.EBI TBA
9548853 5 Isolation of 1-Methylherbipoline Salts of Halisulfate-1 and of Suvanine as Serine Protease Inhibitors from a Marine Sponge, Coscinoderma mathewsiEBI Aoyama Gakuin University
24102612 105 Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.EBI University of Bari "Aldo Moro"
23466230 1 Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate.EBI China Pharmaceutical University
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
23416003 52 Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.EBI Bristol-Myers Squibb R&D
23376251 32 Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.EBI University of Ljubljana
23294255 114 Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI Philipps University Marburg
23164711 3 On scaffold hopping: challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans.EBI Virginia Commonwealth University
11585448 12 Statistical molecular design, parallel synthesis, and biological evaluation of a library of thrombin inhibitors.EBI AstraZeneca
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
7401110 109 Thrombin inhibitors. 2. Amide derivatives of N alpha-substituted L-arginine.EBI TBA
7401109 32 Thrombin inhibitors. 1. Ester derivatives of N alpha-(arylsulfonyl)-L-arginine.EBI TBA
7452681 81 Thrombin inhibitors. 3. Carboxyl-containing amide derivatives of N alpha-substituted L-arginine.EBI TBA
12565961 118 Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.EBI Berlex Biosciences
23124213 4 Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis.EBI University of Ljubljana
22494098 8 Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2).EBI caprotec bioanalytics GmbH
21381769 56 Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI Universite£ de Sherbrooke
22882079 26 Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.EBI Aarhus University
22788964 2 Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.EBI Virginia Commonwealth University
23026080 146 Active site mapping of trypsin, thrombin and matriptase-2 by sulfamoyl benzamidines.EBI University of Bonn
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
22612268 12 Ligand binding stepwise disrupts water network in thrombin: enthalpic and entropic changes reveal classical hydrophobic effect.EBI Philipps University Marburg
22950366 6 Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.EBI Hokkaido University
23043765 1 Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity.EBI China Pharmaceutical University
22726924 14 Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.EBI AstraZeneca
22770607 54 Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.EBI Virginia Commonwealth University
22276953 63 A new strategy for the development of highly potent and selective plasmin inhibitors.EBI Philipps University Marburg
20503967 138 Factor Xa inhibitors: next-generation antithrombotic agents.EBI Bristol-Myers Squibb Company
20561792 4 Development of tryptase inhibitors derived from thalidomide.EBI The University of Tokyo
19682894 2 Photoregulation of thrombin aptamer activity using Bhc caging strategy.EBI University of Science and Technology of China
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 Company, Ltd
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
9599274 4 Cyclotheonamides E2 and E3, new potent serine protease inhibitors from the marine sponge of the genus Theonella.EBI The University of Tokyo
18420408 24 Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.EBI Johnson& Johnson Pharmaceutical Research& Development
18164204 24 Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.EBI Takeda Pharmaceutical Co., Ltd
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 Co., Ltd
18291642 20 Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.EBI Merck Research Laboratories
18289852 22 Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs.EBI Universit£ de Montr£al
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 Company
16876411 17 Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.EBI Daiichi Asubio Medical Research Laboratories, LLC
16460939 25 Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety.EBI Abbott GmbH& Co. KG
16517159 45 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.EBI Abbott GmbH& Co. KG
16289811 56 The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.EBI Pfizer Global Research and Development
16290930 23 Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.EBI Universit£ de Montr£al
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
15837303 52 Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI Berlex Biosciences
15911253 25 P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.EBI Merck Research Laboratories
15261287 44 Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.EBI Central Pharmaceutical Research Institute
15163182 47 Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.EBI Merck Research Laboratories
12646027 43 Synthesis of novel thrombin inhibitors. Use of ring-closing metathesis reactions for synthesis of P2 cyclopentene- and cyclohexenedicarboxylic acid derivatives.EBI Link£ping University
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
12954057 113 Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.EBI Pharmacia Corporation
12954052 25 Synthesis and SAR of thrombin inhibitors incorporating a novel 4-amino-morpholinone sscaffold: analysis of X-ray crystal structure of enzyme inhibitor complex.EBI Link£ping University
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 Ltd.
12408710 2 Thrombin inhibition by novel benzamidine derivatives: a free-energy perturbation study.EBI Universidade Federal do Rio de Janeiro
12238922 28 Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.EBI Research and Development
12036356 234 Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.EBI Berlex Biosciences
12036355 36 Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.EBI University of Parma
11297451 21 Estimation of binding affinities for selective thrombin inhibitors via Monte Carlo simulations.EBI Yale University
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 Company
10794696 233 Protease inhibitors: synthesis and QSAR study of novel classes of nonbasic thrombin inhibitors incorporating sulfonylguanidine and O-methylsulfonylisourea moieties at P1.EBI Universit£ degli Studi
10794688 16 New proline mimetics: synthesis of thrombin inhibitors incorporating cyclopentane- and cyclopentenedicarboxylic acid templates in the P2 position. Binding conformation investigated by X-ray crystallography.EBI Link£ping University
10669559 180 Protease inhibitors: current status and future prospects.EBI University of Queensland
10956211 14 GRID/CPCA: a new computational tool to design selective ligands.EBI Boehringer Ingelheim Pharma KG
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
10464012 5 New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.EBI Rh£ne-Poulenc Rorer
10425086 83 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.EBI DuPont Pharmaceuticals Company
9464370 28 Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.EBI Merck Research Laboratories
9836616 92 Tetrahydro-isoquinoline-based factor Xa inhibitors.EBI Boehringer Mannheim GmbH
9622548 8 Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.EBI 3-Dimensional Pharmaceuticals Inc.
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
9171870 4 Synthesis and pharmacological properties of a close analogue of an antithrombotic pentasaccharide (SR 90107A/ORG 31540).EBI Sanofi Recherche
9154975 5 Binding affinities for sulfonamide inhibitors with human thrombin using Monte Carlo simulations with a linear response method.EBI Yale University
8759623 31 Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.EBI R. W. Johnson Pharmaceutical Research Institute
7966150 60 Design and synthesis of potent and highly selective thrombin inhibitors.EBI F. Hoffmann-La Roche Ltd.
8478905 53 Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.EBI University of Arkansas
1527787 11 Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.EBI Thrombosis Research Institute
3625715 18 Anticoagulant peptides: nature of the interaction of the C-terminal region of hirudin with a noncatalytic binding site on thrombin.EBI TBA
15081015 46 Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
14980679 30 Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.EBI Maxim Pharmaceuticals
15203151 54 Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.EBI 3-Dimensional Pharmaceuticals, Inc.
12873514 56 Design and synthesis of potent and selective macrocyclic thrombin inhibitors.EBI Merck Research Laboratories
12824035 39 Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.EBI Pharmacia Corporation
12781189 6 D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.EBI BASF AG
11909707 69 Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.EBI Life Science R&D, LGCI
11858993 60 Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.EBI Corvas International, Inc.
12270173 23 Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.EBI Universit£ de Montr£al
12039564 1 Solid-phase synthesis of thrombin inhibitors.EBI BASF AG
11738570 29 Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
11738569 26 Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
11459667 13 Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.EBI Medical University of South Carolina
10698459 41 The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.EBI DuPont Pharmaceuticals Company
10698445 11 Exploring the chiral space within the active site of alpha-thrombin with a constrained mimic of D-Phe-Pro-Arg--design, synthesis, inhibitory activity, and X-ray structure of an enzyme-inhibitor complex.EBI Universit£ de Montr£al
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
10340604 22 Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.EBI Research and Development
10201829 9 1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.EBI NV Organon
10498204 25 Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.EBI Rh£ne-Poulenc Rorer
10450972 3 Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.EBI Institute of Chemistry
10450962 4 Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics.EBI University of Illinois at Chicago
9873373 20 Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).EBI Institute for Drug Research
22365562 154 Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.EBI University of Ljubljana
22285569 107 Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).EBI University of Antwerp
22192588 9 Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.EBI Sanofi Pharmaceuticals
22094280 3 Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases.EBI University of Heidelberg
22055408 12 Conformationally restricted analogs of the direct thrombin inhibitor FM 19.EBI University of Michigan
22047802 8 The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.EBI Universit£t Bielefeld
22041058 44 Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI Bristol-Myers Squibb Company
21995444 32 Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.EBI Astellas Pharma Inc
21923104 12 HLE-inhibitory alkaloids with a polyketide skeleton from the marine-derived fungus Coniothyrium cereale.EBI University of Bonn
21807511 13 Synthesis and biochemical evaluation of triazole/tetrazole-containing sulfonamides against thrombin and related serine proteases.EBI The Johns Hopkins University
21795054 8 Thermodynamic and biological evaluation of a thrombin binding aptamer modified with several unlocked nucleic acid (UNA) monomers and a 2'-C-piperazino-UNA monomer.EBI University of Southern Denmark
21714536 25 Rational design of potent, small, synthetic allosteric inhibitors of thrombin.EBI Virginia Commonwealth University
21757348 12 Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities.EBI University of Ljubljana
21741848 66 Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.EBI Universit£ degli Studi di Firenze
21741839 83 Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.EBI Philipps University Marburg
21641796 30 Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.EBI Technical University of Denmark
21295467 22 Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.EBI Merck Research Laboratories
21295466 21 P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.EBI Merck Research Laboratories
21168329 47 New furin inhibitors based on weakly basic amidinohydrazones.EBI Philipps University Marburg
21035339 16 Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.EBI Université de Montréal
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 Ltd
20684597 19 Identification of the first low-molecular-weight inhibitors of matriptase-2.EBI University of Bonn
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 Company Ltd.
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
20028081 2 Micropeptins from an Israeli fishpond water bloom of the cyanobacterium Microcystis sp.EBI Tel-Aviv University
20148533 41 Enhancement of hydrophobic interactions and hydrogen bond strength by cooperativity: synthesis, modeling, and molecular dynamics simulations of a congeneric series of thrombin inhibitors.EBI The State University of New York
20100660 28 Phenyltriazolinones as potent factor Xa inhibitors.EBI Bristol-Myers Squibb
20038105 50 Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.EBI Philipps University Marburg
19674897 21 From natural products to achiral drug prototypes: potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs.EBI Universit£ de Montr£al
19541481 57 Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI Bristol-Myers Squibb Company
19200624 32 Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.EBI F Hoffmann - La Roche Ltd
19447619 3 Preparation of L-proline based aeruginosin 298-A analogs: optimization of the P1-moiety.EBI University of New Orleans
19181521 69 Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor.EBI Universit£ Montpellier 1
19193009 25 Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation.EBI University of Bari
19297158 30 Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.EBI Millennium Pharmaceuticals, Inc
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, Inc
19250826 100 Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.EBI The Medicines Company (Leipzig) GmbH
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 Co., Ltd.
19036586 128 Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.EBI Curacyte Discovery GmbH
18729445 70 3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.EBI University of Ljubljana
18674905 58 Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.EBI Chugai Pharmaceutical Co., Ltd
18667303 27 Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.EBI Kissei Pharmaceutical Co., Ltd
18570365 29 The many roles for fluorine in medicinal chemistry.EBI Merck Research Laboratories
18550370 33 Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.EBI Bristol-Myers Squibb Company
18507371 24 Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.EBI Takeda Pharmaceutical Co., Ltd.
18457385 41 Recent developments in fragment-based drug discovery.EBI Astex Therapeutics Ltd.
18412326 16 Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.EBI University of Ljubljana
17950494 2 Structure of a novel thrombin inhibitor with an uncharged D-amino acid as P1 residue.EBI Institut für Biochemie
15332844 8 Dysinosins B-D, inhibitors of factor VIIa and thrombin from the Australian sponge Lamellodysidea chlorea.EBI Griffith University
11908961 3 Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge.EBI Kirin Brewery Co., Ltd.
9834152 29 Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.EBI National University of Singapore
9834145 5 Isolation of translactone-containing triterpenes with thrombin inhibitory activities from the leaves of Lantana camara.EBI GlaxoWellcome Research and Development
17933529 35 Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17889527 18 2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.EBI Johnson & Johnson
17883259 17 Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.EBI Chinese Academy of Sciences
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 Company
17566736 60 Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.EBI Pfizer Global Research and Development
17555959 27 Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.EBI Daiichi Pharmaceutical Co., Ltd
17462889 110 From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.EBI Curacyte Discovery GmbH
17428662 16 Structure-based organic synthesis of unnatural aeruginosin hybrids as potent inhibitors of thrombin.EBI Université de Montréal
17420122 18 Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI GlaxoSmithKline
17416533 39 Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.EBI Astellas Pharma Inc.
17336062 3 Sulfonamide-related conformational effects and their importance in structure-based design.EBI GlaxoSmithKline
17064913 29 Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.EBI Astellas Pharma Inc.
17010480 21 Synthesis and evaluation of a small library of graftable thrombin inhibitors derived from (L)-arginine.EBI Université catholique de Louvain
16970403 74 Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.EBI University of Antwerp
16913694 46 Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.EBI Institut de Recherches Servier
16793264 13 Potent 4-amino-5-azaindole factor VIIa inhibitors.EBI Celera Genomics
16725321 13 Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.EBI Celera Genomics
16714109 40 Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.EBI Celera
16540315 23 Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.EBI Mochida Pharmaceutical Co., Ltd
16460935 39 A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.EBI Johnson & Johnson Pharmaceutical Research and Development
16413781 13 Investigation of mechanism-based thrombin inhibitors: Implications of a highly conserved water molecule for the binding of coumarins within the S pocket.EBI University of Namur
16302799 2 3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa.EBI University of Namur
16257204 37 Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.EBI Celera
16257203 24 Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles.EBI Merck Research Laboratories
16213711 37 Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16202582 10 Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.EBI National Research Council of Canada
16137886 88 Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.EBI Merck Research Laboratories
15801822 28 9-hydroxyazafluorenes and their use in thrombin inhibitors.EBI Merck Research Laboratories
15501047 75 Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI Merck KGaA
15456260 21 Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element.EBI Daiichi Pharmaceutical Co. Ltd
15341970 59 P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.EBI Lilly Research Laboratory
15261262 10 Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.EBI Merck Research Laboratories
15203158 84 Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI Merck KGaA
15203149 72 Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.EBI Aventis Pharma Deutschland GmbH
15149685 55 Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.EBI University of Ljubljana
15149645 92 Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.EBI Abbott Laboratories
15149641 44 A novel series of potent and selective small molecule inhibitors of the complement component C1s.EBI 3-Dimensional Pharmaceuticals Inc
15125963 20 Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.EBI Daiichi Pharmaceutical Co. Ltd
15115382 16 Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.EBI University of Antwerp
15081014 12 Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
15080981 72 N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
15013007 319 Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.EBI Millennium Pharmaceuticals, Inc.
15013006 69 Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.EBI Millennium Pharmaceuticals, Inc.
15006404 56 Thrombin inhibitors built on an azaphenylalanine scaffold.EBI University of Ljubljana
14980671 78 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.EBI Millennium Pharmaceuticals Inc.
14980670 107 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.EBI Millennium Pharmaceuticals Inc.
14761180 31 Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.EBI Johnson & Johnson Pharmaceutical Research & Development
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 28 Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
14552766 12 Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.EBI Pharmacia Corporation
14521407 87 Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.EBI GlaxoSmithKline Research and Development
14505652 45 Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.EBI Merck Research Laboratories
12951087 23 Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.EBI University of Ljubljana
12824026 13 Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.EBI Pharmacia Corporation
12824021 39 Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.EBI Boehringer Ingelheim Pharma KG
12824020 31 Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI Boehringer Ingelheim Pharma KG
12723948 30 Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.EBI Ajinomoto Company Inc.
12672230 22 Generation of ligand conformations in continuum solvent consistent with protein active site topology: application to thrombin.EBI Thrombosis Research Institute
12668020 29 Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals, Inc.
12668013 42 Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.EBI Aventis Pharma Deutschland GmbH
12668009 36 High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition.EBI Molecumetics
12668008 34 3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.EBI Merck Research Laboratories
12657281 29 Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.EBI Merck Research Laboratories
12643903 72 Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.EBI Bristol-Myers Squibb Co.
12639568 52 Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.EBI Millennium Pharmaceuticals Inc.
12639567 130 Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI Millennium Pharmaceuticals Inc.
12617893 28 Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.EBI Merck Research Laboratories
12617892 43 Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.EBI University of Ljubljana
12593666 30 Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI Senju Pharmaceutical Co.
12593648 53 Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.EBI Aventis Pharmaceuticals
12570369 60 Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.EBI Merck Research Laboratories
12565972 69 Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
12565931 37 Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.EBI Bristol-Myers Squibb Co.
12482444 38 Design and synthesis of factor Xa inhibitors and their prodrugs.EBI Millennium Pharmaceuticals, Inc.
12482415 30 Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.EBI Merck Research Laboratories
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
12113838 36 Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.EBI Millennium Pharmaceuticals, Inc.
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
12039587 39 Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.EBI Aventis Pharmaceuticals
12039586 42 Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.EBI Aventis Pharmaceuticals
12039584 59 Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
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, Inc.
12036353 38 Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.EBI Pfizer Global Research and Development
12031331 48 Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.EBI Millennium Pharmaceuticals, Inc.
11965378 78 Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.EBI Berlex Biosciences
11965377 66 Design and synthesis of aminophenol-based factor Xa inhibitors.EBI Berlex Biosciences
11960487 30 Structure-based design of novel potent nonpeptide thrombin inhibitors.EBI Boehringer Ingelheim Pharma KG
11958994 31 Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.EBI Aventis Pharmaceuticals
11934589 57 Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.EBI Corvas International, Inc.
11881991 21 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.EBI Protherics Molecular Design
11844691 107 4-amidinobenzylamine-based inhibitors of urokinase.EBI Universitat Jena
11814787 73 Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).EBI Merck Research Laboratories
11754575 51 Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxohexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 2. Potency and chirality.EBI GlaxoSmithKline Research and Development
11720865 11 Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues.EBI Shire BioChem Inc.
11689072 49 Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.EBI Axys Pharmaceuticals Inc.
11677132 65 Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.EBI COR Therapeutics, Inc.
11549459 4 Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.EBI National Cancer Institute
11527714 66 Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.EBI COR Therapeutics, Inc.
11527709 19 Optimization of a screening lead for factor VIIa/TF.EBI Axys Pharmaceuticals, Inc.
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 Inc.
11459634 94 Development of potent and selective factor Xa inhibitors.EBI Axys Pharmaceuticals, Inc.
11425539 23 Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI Shionogi & Co., Ltd.
11425524 45 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, Inc.
11378359 57 Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.EBI 3-Dimensional Pharmaceuticals Inc.
11311057 15 Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase.EBI Georgetown University Medical Center
11297447 18 Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.EBI The R. W. Johnson Pharmaceutical Research Institute
11266180 73 The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.EBI Prosthetics Molecular Design
11266160 57 Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.EBI DuPont Pharmaceuticals Company
11212093 21 Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.EBI BioChem Pharma Inc.
11206465 13 Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.EBI Aventis Pharma
11133089 28 Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.EBI LG Chemical Ltd
11087570 14 Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 1. The alpha-methyl-trans-lactam template.EBI Glaxo Wellcome Research and Development
11087565 86 Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.EBI DuPont Pharmaceuticals Company
11078188 20 1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.EBI Shionogi & Co., Ltd
11078187 36 Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI Shionogi & Co., Ltd
11063603 53 Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.EBI Pfizer Global Research and Development
11055356 179 Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.EBI Axys Pharmaceuticals, Inc.
11055355 72 Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.EBI Axys Pharmaceuticals, Inc.
11055344 37 Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.EBI Corvas International, Inc.
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
10866393 24 Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.EBI DuPont Pharmaceuticals Company
10853669 102 Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI Berlex Biosciences
10853668 52 Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.EBI Berlex Biosciences
10843219 20 Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.EBI Merck Research Laboratories
10782677 72 Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI Corvas International, Inc.
10782664 42 Isoxazolines and isoxazoles as factor Xa inhibitors.EBI The DuPont Pharmaceuticals Company
10698439 68 Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI Rhone-Poulenc Rorer
10669563 7 Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1.EBI Warner-Lambert Company
10639283 135 Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.EBI Berlex Biosciences
10636250 20 Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.EBI 3-Dimensional Pharmaceuticals
10636249 21 Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor.EBI 3-Dimensional Pharmaceutical, Inc.
10636232 58 Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence.EBI COR Therapeutics, Inc.
10636229 27 Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals
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, Inc.
10612586 14 Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.EBI Yoshitomi Pharmaceutical Industries, LTD.
10560742 85 3-Amidinophenylalanine-based inhibitors of urokinase.EBI Universität Jena
10543886 1 Two-stage method for protein-ligand docking.EBI German National Research Center for Information Technology
10509929 116 Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI Rhône-Poulenc Rorer
10498222 3 Asymmetric synthesis of novel quaternary alpha-hydroxy-delta-lactam dipeptide surrogates.EBI Corvas International, Inc.
10498211 42 Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI Corvas International, Inc.
10498197 58 The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.EBI Warner-Lambert Company
10498196 42 The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.EBI Warner-Lambert Company
10498193 22 Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.EBI Biotech Research Institute
10447955 16 Potent bivalent thrombin inhibitors: replacement of the scissile peptide bond at P(1)-P(1)' with arginyl ketomethylene isosteres.EBI National Research Council Canada
10425106 12 4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.EBI Brown University
10425087 110 Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.EBI DuPont Pharmaceuticals Company
10397495 49 Thrombin inhibitors based on [5,5] trans-fused indane lactams.EBI Glaxo Wellcome Research and Development
10346927 114 Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI Berlex Biosciences
10340621 17 Optimisation of the P2 pharmacophore in a series of thrombin inhibitors: ion-dipole interactions with lysine 60G.EBI Novartis Horsham Research Center
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
10230612 22 Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.EBI DuPont Pharmaceuticals Company
10230610 12 Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.EBI BioChem Therapeutic Inc.
10212123 5 Bound structures of novel P3-P1' beta-strand mimetic inhibitors of thrombin.EBI Michigan State University
10212122 35 Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI Molecumetics Ltd.
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, Inc.
10206546 23 Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications.EBI Warner-Lambert Company
10201846 17 Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.EBI Lilly Research Laboratories
10201839 22 Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.EBI Novartis Horsham Research Center
10091697 6 Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin.EBI Glaxo Wellcome Research and Development
9934479 17 Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.EBI NV Organon Scientific Development Group
9934475 30 The discovery of orally available thrombin inhibitors: studies towards the optimisation of CGH1668.EBI Novartis Horsham Research Center
9876114 111 Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.EBI Institut für Biochemie
9873743 12 Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.EBI Warner-Lambert Company
9873701 27 Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications.EBI BioChem Therapeutic Inc.
9873692 54 Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI DuPont Pharmaceuticals Company
9873654 37 5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.EBI GlaxoWellcome Research and Development
9873607 21 The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.EBI DuPont Pharmaceuticals Company
9873581 21 Benzylamine-based selective and orally bioavailable inhibitors of thrombin.EBI Biotech Research Institute
9873569 16 Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI Corvas International, Inc.
9873562 3 Templates for design of inhibitors for serine proteases: application of the program DOCK to the discovery of novel inhibitors for thrombin.EBI Wayne State University
9873535 12 Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.EBI Molecumetics Ltd.
9873520 27 Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.EBI Berlex Biosciences
9873422 16 C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.EBI Merck Research Laboratories
9873418 16 Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.EBI Merck Research Laboratories
9873414 13 Potent and efficacious thienylamidine-incorporated thrombin inhibitors.EBI Biotech Research Institute
9873411 103 Identification of a potent analogue of Nazumamide A through iteration of combinatorial tetrapeptide libraries.EBI Central Drug Research Institute
9873400 12 Diarylsulfonamides as selective, non-peptidic thrombin inhibitors.EBI Pharmazeutisch-Chemisches Institut der Universität
9873397 37 In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals
9871744 5 1,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors.EBI Menarini Ricerche S.p.A.
9871680 5 Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.EBI ProScript, Inc.
9871674 34 Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.EBI DuPont Merck Pharmaceutical Company
9871573 15 Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI Biotech Research Institute
9871547 15 L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.EBI Merck Research Laboratories
9871540 100 Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.EBI DuPont Merck Pharmaceutical Company
9871532 8 Solid phase synthesis of benzylamine-derived sulfonamide library.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
9804686 16 Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.EBI Merck Research Laboratories
9784099 84 Design of benzamidine-type inhibitors of factor Xa.EBI Institut für Biochemie
9767628 31 Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.EBI GlaxoWellcome Medicines Research Centre
9733491 21 Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.EBI Novartis Pharma AG
9733480 93 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.EBI Berlex Biosciences
9733479 18 (Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.EBI Berlex Biosciences
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
9544200 24 Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.EBI Merck Research Laboratories
9484495 74 Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.EBI Collegeville
9438022 55 Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.EBI DuPont Merck Pharmaceutical Company
9371237 69 Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.EBI Merck Research Laboratories
9341916 30 Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.EBI Rhône-Poulenc Rorer
9301672 18 Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.EBI Chinese Academy of Sciences
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
8917639 50 Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.EBI Corvas International, Inc.
8917638 26 Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.EBI Corvas International Inc.
8515421 6 The solution conformation of (D)Phe-Pro-containing peptides: implications on the activity of Ac-(D)Phe-Pro-boroArg-OH, a potent thrombin inhibitor.EBI Du Pont Merck Pharmaceutical Company
8426361 111 Highly selective tripeptide thrombin inhibitors.EBI Lilly Research Laboratories
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
8164262 38 Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.EBI Daiichi Pharmaceutical Company, Ltd.
8035417 23 Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
7966143 5 Binding of fluorescent and spin-labeled C-terminal hirudin analogs to thrombin.EBI Ohio State University
7739010 118 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI Thrombosis Research Institute
7629790 32 New orally active serine protease inhibitors.EBI Minase Research Institute
7562931 41 Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.EBI ZENECA Pharmaceuticals
7473571 90 Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI Lilly Research Laboratories
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
1527782 8 Synthesis of a homologous series of ketomethylene arginyl pseudodipeptides and application to low molecular weight hirudin-like thrombin inhibitors.EBI National Research Council of Canada
1447734 19 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
22299583 34 Tripeptides with non-code amino acids as potential serine proteases inhibitors.BDB Medical University of Bialystok
21981000 104 Polyphenol fatty acid esters as serine protease inhibitors: a quantum-chemical QSAR analysis.BDB Slovak University of Technology
20030517 18 Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.BDB Medical University of Bialystok
9203642 14 Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor.BDB Schering-Plough Research Institute
9195869 28 Molecular recognition at the thrombin active site: structure-based design and synthesis of potent and selective thrombin inhibitors and the X-ray crystal structures of two thrombin-inhibitor complexes.BDB Laboratorium für Organische Chemie
19520086 27 Think twice: understanding the high potency of bis(phenyl)methane inhibitors of thrombin.BDB Philipps-University Marburg
19409795 186 Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores.BDB BioCryst Pharmaceuticals
19371038 37 Compounds binding to the S2-S3 pockets of thrombin.BDB University of Kalmar
16821772 270 Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.BDB Curacyte Chemistry GmbH
17850059 195 N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.BDB Montana State University
18459730 144 Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.BDB University of Namur
17985858 27 Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.BDB Georgetown University Medical Center
17914785 67 Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa.BDB Bristol-Myers Squibb Company
14521405 29 Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.BDB Bristol-Myers Squibb Company
11342132 24 Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors.BDB Boehringer Ingelheim Pharma KG
17227710 141 Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa.BDB Berlex
17536795 118 Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors(1).BDB Berlex Biosciences
9468142 60 Design of potent selective zinc-mediated serine protease inhibitors.BDB Arris
15261268 26 Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.BDB Aventis Pharma Deutschland GmbH
15261269 35 Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.BDB Aventis Pharma Deutschland GmbH
16621549 40 Novel 5-azaindole factor VIIa inhibitors.BDB Celera
15632123 9 A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.BDB Genentech
13678408 30 Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors.BDB Pharmacia Corporation
12954058 193 Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.BDB Pharmacia Corporation
14561089 6 Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.BDB Pharmacia Corporation
15522303 73 Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).BDB Celera
12742021 191 Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.BDB Celera
10779411 24 Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.BDB Axys Pharmaceutical
11731301 192 Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.BDB Axys Pharmaceutical
15771442 154 In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.BDB Johnson & Johnson Pharmaceutical
10966741 12 Crystal structures of human factor Xa complexed with potent inhibitors.BDB Aventis Pharma
11292354 48 A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.BDB Axys Pharmaceuticals Corporation
12061878 100 Design and quantitative structure-activity relationship of 3-amidinobenzyl-1H-indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa.BDB Aventis Pharma Deutschland GmbH
16460932 27 Discovery of novel heterocyclic factor VIIa inhibitors.BDB Celera
15857135 128 Structural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.BDB Aventis Pharma Deutschland GmbH
16621574 28 Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.BDB F. Hoffmann-La Roche Ltd.
15664864 44 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.BDB F. Hoffmann-La Roche Ltd.
16213138 80 Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.BDB F. Hoffmann-La Roche Ltd.
17181160 82 Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.BDB Daiichi Asubio Medical Research Laboratories LLC (DAIAMED)
16870435 29 Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
16682200 41 Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.BDB Bristol-Myers Squibb Company
15771420 58 Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
12593649 15 Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.BDB Aventis Pharma
16480269 9 Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors.BDB Astex