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153 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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
23294255 114 Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI Philipps University Marburg
10602702 22 Simple linear QSAR models based on quantum similarity measures.EBI Czech Academy of Sciences
3514912 48 Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates.EBI TBA
22726924 14 Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV.EBI AstraZeneca
16250649 10 Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.EBI Brown 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
12930148 41 Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.EBI Johnson& Johnson Pharmaceutical Research& Development
12190311 37 Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).EBI GSK
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
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
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
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
2319567 29 Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia.EBI University of North Carolina
15081015 46 Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
12873514 56 Design and synthesis of potent and selective macrocyclic thrombin inhibitors.EBI Merck Research Laboratories
10698459 41 The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.EBI DuPont Pharmaceuticals Company
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
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
9873373 20 Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).EBI Institute for Drug Research
19841155 29 MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.EBI Merck Research Laboratories
 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
 32 Bisbenzamidine isoxazoline derivatives as factor Xa inhibitorsEBI TBA
 27 Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogatesEBI TBA
 44 Biaryl substituted alkylboronate esters as thrombin inhibitorsEBI TBA
 3 An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatranEBI TBA
 25 Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogatesEBI TBA
 14 RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLESEBI 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
15801822 28 9-hydroxyazafluorenes and their use in thrombin inhibitors.EBI Merck Research Laboratories
15203158 84 Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI Merck KGaA
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
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
14505652 45 Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.EBI Merck Research Laboratories
12824026 13 Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.EBI Pharmacia Corporation
12824020 31 Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI Boehringer Ingelheim Pharma KG
12668020 29 Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI 3-Dimensional Pharmaceuticals, Inc.
12668008 34 3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.EBI Merck Research Laboratories
12643903 72 Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.EBI Bristol-Myers Squibb Co.
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
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.
12113838 36 Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.EBI Millennium Pharmaceuticals, Inc.
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
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.
11844691 107 4-amidinobenzylamine-based inhibitors of urokinase.EBI Universitat Jena
11677132 65 Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.EBI COR Therapeutics, Inc.
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.
11378359 57 Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.EBI 3-Dimensional Pharmaceuticals Inc.
11266180 73 The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.EBI Prosthetics Molecular Design
11212093 21 Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors.EBI BioChem Pharma Inc.
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
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
10866385 13 Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.EBI The Oxford Centre for Molecular Sciences
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.
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
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.
10509929 116 Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI Rhône-Poulenc Rorer
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
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
10328312 27 Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.EBI DuPont Pharmaceuticals Company
10328293 23 The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore.EBI Novartis Horsham Research Centre
10230612 22 Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.EBI DuPont Pharmaceuticals Company
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
10206542 50 Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.EBI Warner-Lambert Company
10091694 90 Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.EBI Nippon Steel Corporation
9934495 26 Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.EBI Corvas International, Inc.
9873743 12 Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.EBI Warner-Lambert 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
9873569 16 Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI Corvas International, Inc.
9873535 12 Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.EBI Molecumetics Ltd.
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
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
9804686 16 Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.EBI Merck Research Laboratories
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
9438022 55 Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.EBI DuPont Merck Pharmaceutical Company
9379436 46 Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.EBI ZENECA Pharmaceuticals
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.
8426361 111 Highly selective tripeptide thrombin inhibitors.EBI Lilly Research Laboratories
8035417 23 Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
7629790 32 New orally active serine protease inhibitors.EBI Minase Research Institute
7562936 10 Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin.EBI Friedrich Miescher-Institut
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
2136920 39 New leupeptin analogues: synthesis and inhibition data.EBI University of Arkansas
22299583 34 Tripeptides with non-code amino acids as potential serine proteases inhibitors.BDB Medical University of Bialystok
20429779 11 Carbocyclic potential DNA minor groove binders and their biological evaluation.BDB Medical University
20030517 18 Synthesis and activity of amides of tripeptides as potential urokinase inhibitors.BDB Medical University of Bialystok
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
9468142 60 Design of potent selective zinc-mediated serine protease inhibitors.BDB Arris
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