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104 articles for thisTarget


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

PMID
Data
Article Title
Organization
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.EBI
Bristol-Myers Squibb
Novel phenylalanine derived diamides as Factor XIa inhibitors.EBI
Bristol-Myers Squibb
Pyridine and pyridinone-based factor XIa inhibitors.EBI
Bristol-Myers Squibb
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.EBI
Bristol-Myers Squibb
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.EBI
Rempex Pharmaceuticals
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI
Bristol-Myers Squibb
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.EBI
Bristol-Myers Squibb
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.EBI
Bristol-Myers Squibb
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.EBI
Sanofi-Aventis R&D
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.EBI
Bristol-Myers Squibb Research & Development
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.EBI
Lg Life Sciences
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
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI
Philipps University Marburg
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
2-Amidino analogs of glycine-amiloride conjugates: inhibitors of urokinase-type plasminogen activator.EBI
University Of Louisville
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
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI
Johnson & Johnson Pharmaceutical Research & Development
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.EBI
Bristol-Myers Squibb Research And Development
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.EBI
University Of Antwerp
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
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.EBI
Abbott
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
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
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
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI
Rh£Ne-Poulenc Rorer
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.EBI
Merck Research Laboratories
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
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.EBI
Klinikum Der Friedrich-Schiller-Universit£T Jena
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
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.EBI
Merck Research Laboratories
 
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitorEBI
TBA
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).EBI
University Of Antwerp
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI
Bristol-Myers Squibb
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.EBI
University Of Basel
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor.EBI
Takeda Pharmaceutical
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
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.EBI
National Human Genome Research Institute
Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).EBI
Berlex Biosciences
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI
Bristol-Myers Squibb
 
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogatesEBI
TBA
 
(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitorsEBI
TBA
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.EBI
Millennium Pharmaceuticals
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
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
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Geometry of GPPE binding to picrate and to the urokinase type plasminogen activator.EBI
Pedagogical University
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
Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI
Glaxosmithkline
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.EBI
University Of Antwerp
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.EBI
Johnson & Johnson Pharmaceutical Research And Development
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.EBI
Merck Research Laboratories
9-hydroxyazafluorenes and their use in thrombin inhibitors.EBI
Merck Research Laboratories
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.EBI
Abbott Laboratories
Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.EBI
Wyeth Research
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.EBI
Pfizer
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.EBI
Abbott Laboratories
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.EBI
University Of Antwerp
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.EBI
The Bristol-Myers Squibb Pharmaceutical Research Institute
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
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.EBI
Millennium Pharmaceuticals
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs.EBI
Millennium Pharmaceuticals
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
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.EBI
Millennium Pharmaceuticals
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
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.EBI
The Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI
Celera
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.EBI
Celera
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Structure-based design of novel potent nonpeptide thrombin inhibitors.EBI
Boehringer Ingelheim Pharma
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors.EBI
Aventis Pharmaceuticals
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines.EBI
Pfizer
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.EBI
Pfizer
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.EBI
Axys Pharmaceuticals
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.EBI
Cor Therapeutics
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
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.EBI
3-Dimensional Pharmaceuticals
Nonbenzamidine compounds as selective factor Xa inhibitors.EBI
Aventis Pharmaceuticals
Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.EBI
Corvas International
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI
Rhone-Poulenc Rorer
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI
RhôNe-Poulenc Rorer
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
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
Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.EBI
Dupont Pharmaceuticals
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI
Biotech Research Institute
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
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
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.EBI
Eli Lilly
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
 
Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazolesBDB
Hacettepe University
3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.BDB
Jilin University