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89 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
1433218 3 Guanidinophenyl-substituted enol lactones as selective, mechanism-based inhibitors of trypsin-like serine proteases.EBI University of Illinois
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
15837303 52 Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI Berlex Biosciences
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.
10956211 14 GRID/CPCA: a new computational tool to design selective ligands.EBI Boehringer Ingelheim Pharma KG
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
8496923 9 New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue.EBI CNRS-CERCOA
2231595 96 Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.EBI Abbott Laboratories
15081015 91 Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI The Bristol-Myers Squibb Pharmaceutical Research Institute
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
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
 34 Peptidyl -keto thiazole as potent thrombin inhibitorsEBI TBA
 22 Design and synthesis of conformationally constrained arginal thrombin inhibitorsEBI TBA
 48 DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORSEBI TBA
 19 Rational design of selective thrombin inhibitorsEBI TBA
 37 Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI TBA
 4 Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitorEBI TBA
 24 Novel thrombin inhibitors that are based on a macrocyclic tripeptide motifEBI TBA
 2 Kinetic characterization of a peptide inhibitor of trypsin isolated from a synthetic peptide combinatorial libraryEBI TBA
 9 Diphenylborinic acid is a strong inhibitor of serine proteasesEBI TBA
 13 Characterization of LY806303 as a potent and selective inhibitor of thrombinEBI TBA
12951087 23 Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.EBI University of Ljubljana
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
12372525 2 A mechanism-based probe for gp120-Hydrolyzing antibodies.EBI University of Texas-Houston Medical School
11965377 66 Design and synthesis of aminophenol-based factor Xa inhibitors.EBI Berlex Biosciences
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
11425539 23 Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI Shionogi & Co., Ltd.
11133089 28 Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.EBI LG Chemical Ltd
11078187 36 Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI Shionogi & Co., Ltd
10853669 102 Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI Berlex Biosciences
10782664 42 Isoxazolines and isoxazoles as factor Xa inhibitors.EBI The DuPont Pharmaceuticals 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
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
10560742 85 3-Amidinophenylalanine-based inhibitors of urokinase.EBI Universität Jena
10508439 4 Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.EBI Washington University
10498193 22 Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.EBI Biotech Research Institute
10346927 114 Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI Berlex Biosciences
10230630 36 Thrombin inhibitors based on a propargylglycine template.EBI Biotech Research Institute
10212122 35 Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI Molecumetics Ltd.
9934479 17 Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.EBI NV Organon Scientific Development Group
9925737 57 N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.EBI Nippon Steel Corporation
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
9873581 21 Benzylamine-based selective and orally bioavailable inhibitors of thrombin.EBI Biotech Research Institute
9873520 27 Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.EBI Berlex Biosciences
9873414 13 Potent and efficacious thienylamidine-incorporated thrombin inhibitors.EBI Biotech Research Institute
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
9544206 94 2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.EBI Warner-Lambert Company
9406602 7 Assessment of solvation effects on calculated binding affinity differences: trypsin inhibition by flavonoids as a model system for congeneric series.EBI Universidad de Alcalá
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
7739010 118 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI Thrombosis Research Institute
7473571 90 Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI 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
2391691 55 Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.EBI Merck Sharp and Dohme Research Laboratories
1447734 29 Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.EBI University of Illinois
10869410 62 S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.BDB Centre de Recherches de Croissy
9802391 31 The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB Uppsala University
9195867 15 Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.BDB University of California Berkeley
20383151 2 Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.BDB Dana-Farber Cancer Institute
19648931 16 Design, synthesis and selection of DNA-encoded small-molecule libraries.BDB Praecis Pharmaceuticals
19305397 22 Molecular docking and ligand specificity in fragment-based inhibitor discovery.BDB University of California, San Francisco
 28 A Thermodynamic Study of the Reactions of Cyclodextrins with Primary and Secondary Aliphatic Alcohols, with D- and L-Phenylalanine, and with L-Phenylalanine AmideBDB NIST
19699645 12 Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.BDB Northern Kentucky University
17184135 28 HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.BDB Rutgers University
14761195 114 Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.BDB University of Athens
10531324 22 Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor.BDB Indian Institute of Science