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88 articles for thisTarget


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

PMID
Data
Article Title
Organization
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI
University Of Florida
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI
Berlex Biosciences
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
GRID/CPCA: a new computational tool to design selective ligands.EBI
Boehringer Ingelheim Pharma
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
Design and synthesis of potent and highly selective thrombin inhibitors.EBI
F. Hoffmann-La Roche
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.EBI
University Of Arkansas
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
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.EBI
Abbott Laboratories
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI
The Bristol-Myers Squibb Pharmaceutical Research Institute
D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.EBI
Basf
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.EBI
Life Science R & D, Lgci
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.EBI
Medical University Of South Carolina
 
Peptidyl -keto thiazole as potent thrombin inhibitorsEBI
TBA
 
Design and synthesis of conformationally constrained arginal thrombin inhibitorsEBI
TBA
 
DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORSEBI
TBA
 
Rational design of selective thrombin inhibitorsEBI
TBA
 
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI
TBA
 
Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitorEBI
TBA
 
Novel thrombin inhibitors that are based on a macrocyclic tripeptide motifEBI
TBA
 
Kinetic characterization of a peptide inhibitor of trypsin isolated from a synthetic peptide combinatorial libraryEBI
TBA
 
Diphenylborinic acid is a strong inhibitor of serine proteasesEBI
TBA
 
Characterization of LY806303 as a potent and selective inhibitor of thrombinEBI
TBA
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.EBI
University Of Ljubljana
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
A mechanism-based probe for gp120-Hydrolyzing antibodies.EBI
University Of Texas-Houston Medical School
Design and synthesis of aminophenol-based factor Xa inhibitors.EBI
Berlex Biosciences
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
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI
Shionogi
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.EBI
Lg Chemical
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI
Shionogi
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI
Berlex Biosciences
Isoxazolines and isoxazoles as factor Xa inhibitors.EBI
Dupont Pharmaceuticals
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.EBI
Berlex Biosciences
Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.EBI
3-Dimensional Pharmaceuticals
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
3-Amidinophenylalanine-based inhibitors of urokinase.EBI
UniversitäT Jena
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.EBI
Washington University
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.EBI
Biotech Research Institute
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI
Berlex Biosciences
Thrombin inhibitors based on a propargylglycine template.EBI
Biotech Research Institute
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors.EBI
Molecumetics
Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety.EBI
Nv Organon Scientific Development Group
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
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
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.EBI
Biotech Research Institute
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.EBI
Berlex Biosciences
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.EBI
Biotech Research Institute
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors.EBI
Novartis Pharma
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
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.EBI
Berlex Biosciences
2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.EBI
Warner-Lambert
Assessment of solvation effects on calculated binding affinity differences: trypsin inhibition by flavonoids as a model system for congeneric series.EBI
Universidad De Alcalá
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.EBI
Merck Research Laboratories
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI
Thrombosis Research Institute
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI
Eli Lilly
Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.EBI
TBA
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.EBI
Merck Sharp And Dohme Research Laboratories
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
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
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB
Uppsala University
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.BDB
University Of California Berkeley
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.BDB
Dana-Farber Cancer Institute
Design, synthesis and selection of DNA-encoded small-molecule libraries.BDB
Praecis Pharmaceuticals
Molecular docking and ligand specificity in fragment-based inhibitor discovery.BDB
University Of California San Francisco
 
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
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.BDB
Northern Kentucky University
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.BDB
Rutgers University
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
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