The first public molecular recognition database, BindingDB supports research, education and practice in drug discovery, pharmacology and related fields.

BindingDB contains 2.8M data for 1.2M Compounds and 9.2K Targets. Of those, 1,346K data for 622K Compounds and 4.5K Targets were curated by BindingDB curators. BindingDB is a FAIRsharing resource.

If BindingDB was of value to your research, please take a moment to donate to this nonprofit project. Your donation will let us provide you with more data and improved service.

Advanced Search

389 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.EBI
Novartis Pharma
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.EBI
Novartis Institutes For Biomedical Research
An efficient anticoagulant candidate: Characterization, synthesis and in vivo study of a fondaparinux analogue Rrt1.17.EBI
Nankai University
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.EBI
Bristol-Myers Squibb
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.EBI
Global Blood Therapeutics
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.EBI
Bristol-Myers Squibb R & D
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.EBI
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.EBI
Bristol-Myers Squibb Research & Development
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.EBI
Bristol-Myers Squibb R & D
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.EBI
Bristol-Myers Squibb Research & Development
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.EBI
Southern Research
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.EBI
Bristol-Myers Squibb
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.EBI
Merck Research Laboratories
Novel phenylalanine derived diamides as Factor XIa inhibitors.EBI
Bristol-Myers Squibb
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.EBI
Aurigene Discovery Technologies
Development of a novel tricyclic class of potent and selective FIXa inhibitors.EBI
Merck Research Laboratories
Development of a novel class of potent and selective FIXa inhibitors.EBI
Merck Research Laboratories
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.EBI
Southeast University
Pyridine and pyridinone-based factor XIa inhibitors.EBI
Bristol-Myers Squibb
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.EBI
TBA
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.EBI
Bristol-Myers Squibb
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.EBI
Institute For Infection Research
Rapid development of two factor IXa inhibitors from hit to lead.EBI
Merck Research Laboratories
Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.EBI
Shenyang Pharmaceutical University
Identification of anthranilamide derivatives as potential factor Xa inhibitors: drug design, synthesis and biological evaluation.EBI
China Pharmaceutical University
Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.EBI
Bristol-Myers Squibb R & D
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.EBI
Bristol-Myers Squibb
Design, synthesis and evaluation of isoxazolo[5,4-d]pyrimidin-4(5H)-one derivatives as antithrombotic agents.EBI
Southeast University
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.EBI
Bristol-Myers Squibb
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system.EBI
Astellas Pharma
A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds.EBI
Virginia Commonwealth University
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates.EBI
Astellas Pharma
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.EBI
Bristol-Myers Squibb
How aß-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
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
Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.EBI
Aventis Pharma Deutschland
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.EBI
Bristol-Myers Squibb
Heterocyclic core analogs of a direct thrombin inhibitor.EBI
Merck Research Laboratories
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.EBI
Astrazeneca
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.EBI
Bristol-Myers Squibb R & D
Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.EBI
Aurigene Discovery Technologies
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
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 &Quot;Aldo Moro&Quot
Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors.EBI
Bristol-Myers Squibb 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
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores.EBI
University Of Ljubljana
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.EBI
Bristol-Myers Squibb
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.EBI
Bristol-Myers Squibb R & D
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
Torsion angle preferences in druglike chemical space: a comprehensive guide.EBI
University Of Hamburg
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI
Philipps University Marburg
Local structural changes, global data views: graphical substructure-activity relationship trailing.EBI
Rheinische Friedrich-Wilhelms-Universita£T
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.EBI
Celera Genomics
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.EBI
Berlex Biosciences
Synopsis of some recent tactical application of bioisosteres in drug design.EBI
Bristol-Myers Squibb Pharmaceutical Research And Development
Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.EBI
Virginia Commonwealth University
Polysulfated xanthones: multipathway development of a new generation of dual anticoagulant/antiplatelet agents.EBI
Universidade Do Porto (Cequimed-Up)
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
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.EBI
Virginia Commonwealth University
A new strategy for the development of highly potent and selective plasmin inhibitors.EBI
Philipps University Marburg
Factor Xa inhibitors: next-generation antithrombotic agents.EBI
Bristol-Myers Squibb
Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis.EBI
Trigen
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
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI
University Of Florida
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.EBI
Bristol-Myers Squibb Research And Development
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Sulfonamidolactam inhibitors of coagulation factor Xa.EBI
Bristol-Myers Squibb
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI
Johnson & Johnson Pharmaceutical Research & Development
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.EBI
Glaxosmithkline
Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.EBI
Daiichi Sankyo
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
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.EBI
Daiichi Asubio Medical Research Laboratories
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.EBI
Abbott
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.EBI
Central Pharmaceutical Research Institute
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors.EBI
Berlex Biosciences
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
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.EBI
Merck Research Laboratories
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
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.EBI
Pharmacia
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
Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.EBI
Berlex Biosciences
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
Protease inhibitors: current status and future prospects.EBI
University Of Queensland
GRID/CPCA: a new computational tool to design selective ligands.EBI
Boehringer Ingelheim Pharma
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.EBI
Rh£Ne-Poulenc Rorer
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
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1.EBI
Dupont Pharmaceuticals
Tetrahydro-isoquinoline-based factor Xa inhibitors.EBI
Boehringer Mannheim
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 biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors.EBI
Thrombosis Research Institute
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.EBI
The Bristol-Myers Squibb Pharmaceutical Research Institute
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.EBI
Maxim Pharmaceuticals
Exploring new non-sugar sulfated molecules as activators of antithrombin.EBI
Virginia Commonwealth University
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.EBI
Pharmacia
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1.EBI
Life Science R & D, Lgci
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds.EBI
Corvas International
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand.EBI
Dupont Pharmaceuticals
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
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.EBI
Research And Development
 
S1 heterocyclic thrombin inhibitorsEBI
TBA
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.EBI
University Of Ljubljana
Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.EBI
Sanofi Pharmaceuticals
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.EBI
Universit£T Bielefeld
Orally active zwitterionic factor Xa inhibitors with long duration of action.EBI
Daiichi Sankyo
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.EBI
Bristol-Myers Squibb
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
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.EBI
Philipps University Marburg
Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.EBI
Technical University Of Denmark
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors.EBI
Daiichi Sankyo
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.EBI
Glaxosmithkline
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.EBI
Glaxosmithkline
2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor.EBI
Daiichi Sankyo
New furin inhibitors based on weakly basic amidinohydrazones.EBI
Philipps University Marburg
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
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
Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors.EBI
Trigen
Phenyltriazolinones as potent factor Xa inhibitors.EBI
Bristol-Myers Squibb
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.EBI
Glaxosmithkline
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.EBI
Philipps University Marburg
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI
Bristol-Myers Squibb
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.EBI
F. Hoffmann-La Roche
Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor.EBI
University Of Montpellier
Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation.EBI
University Of Bari
 
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moietyEBI
TBA
 
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitorsEBI
TBA
 
Bisbenzamidine isoxazoline derivatives as factor Xa inhibitorsEBI
TBA
 
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogatesEBI
TBA
 
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogatesEBI
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
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.EBI
The Medicines Company (Leipzig)
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.EBI
Pfizer
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
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.EBI
Bristol-Myers Squibb
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.EBI
Curacyte Discovery
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
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors.EBI
Daiichi Sankyo
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination.EBI
Chugai Pharmaceutical
Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.EBI
Kissei Pharmaceutical
Synthesis and evaluation of acylguanidine FXa inhibitors.EBI
Bristol-Myers Squibb Research And Development
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
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.EBI
Takeda Pharmaceutical
Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.EBI
University Of Ljubljana
Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.EBI
National University Of Singapore
7-fluoroindazoles as potent and selective inhibitors of factor Xa.EBI
Johnson & Johnson Pharmaceutical Research And Development
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.EBI
Glaxosmithkline
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
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
Aminopyrrolidineamide inhibitors of site-1 protease.EBI
Pfizer
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa.EBI
Pfizer
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors.EBI
Daiichi Pharmaceutical
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.EBI
Curacyte Discovery
Selective and dual action orally active inhibitors of thrombin and factor Xa.EBI
Glaxosmithkline
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.EBI
Astellas Pharma
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.EBI
Astellas Pharma
Potent 4-amino-5-azaindole factor VIIa inhibitors.EBI
Celera Genomics
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.EBI
Celera
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.EBI
Mochida Pharmaceutical
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.EBI
Johnson & Johnson Pharmaceutical Research And Development
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.EBI
Celera
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
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.EBI
Pfizer
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI
Merck
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
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.EBI
Merck
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition.EBI
Aventis Pharma Deutschland
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.EBI
University Of Ljubljana
A novel series of potent and selective small molecule inhibitors of the complement component C1s.EBI
3-Dimensional Pharmaceuticals
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.EBI
Daiichi Pharmaceutical
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
Thrombin inhibitors built on an azaphenylalanine scaffold.EBI
University Of Ljubljana
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
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.EBI
The Bristol-Myers Squibb Pharmaceutical Research Institute
Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations.EBI
Yale University
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.EBI
Pharmacia
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.EBI
Merck
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics.EBI
University Of Ljubljana
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.EBI
Pharmacia
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents.EBI
Boehringer Ingelheim Pharma
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.EBI
Boehringer Ingelheim Pharma
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.EBI
Bristol-Myers Squibb
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids.EBI
Ajinomoto
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.EBI
3-Dimensional Pharmaceuticals
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors.EBI
Aventis Pharma Deutschland
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.EBI
Bristol-Myers Squibb
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics.EBI
University Of Ljubljana
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI
Senju Pharmaceutical
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.EBI
Aventis Pharmaceuticals
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors.EBI
Bristol-Myers Squibb
Design and synthesis of factor Xa inhibitors and their prodrugs.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
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.EBI
Millennium Pharmaceuticals
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
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
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
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors.EBI
Millennium Pharmaceuticals
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
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.EBI
Millennium Pharmaceuticals
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity.EBI
Berlex Biosciences
Design and synthesis of aminophenol-based factor Xa inhibitors.EBI
Berlex Biosciences
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
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.EBI
Corvas International
Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors.EBI
Shire Biochem
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
4-amidinobenzylamine-based inhibitors of urokinase.EBI
Universitat Jena
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
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.EBI
Cor Therapeutics
Optimization of a screening lead for factor VIIa/TF.EBI
Axys Pharmaceuticals
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
Development of potent and selective factor Xa inhibitors.EBI
Axys Pharmaceuticals
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa.EBI
Prosthetics Molecular Design
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core.EBI
Dupont Pharmaceuticals
Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors.EBI
Aventis Pharma
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.EBI
Dupont Pharmaceuticals
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors.EBI
Pfizer
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.EBI
Corvas International
Nonbenzamidine compounds as selective factor Xa inhibitors.EBI
Aventis Pharmaceuticals
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.EBI
Dupont Pharmaceuticals
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.EBI
The University Of Queensland
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.EBI
Berlex Biosciences
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.EBI
Berlex Biosciences
Trypsin inhibitors for the treatment of pancreatitis.EBI
Novartis Pharma
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability.EBI
Astrazeneca
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.EBI
Philipps University Marburg
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.EBI
Corvas International
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.EBI
Chinese Academy Of Sciences
Isoxazolines and isoxazoles as factor Xa inhibitors.EBI
Dupont Pharmaceuticals
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.EBI
Rhone-Poulenc Rorer
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
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.EBI
University Of Wollongong
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
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
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.EBI
RhôNe-Poulenc Rorer
Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities.EBI
Peking University
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations.EBI
Washington University
Novel benzo-fused lactam scaffolds as factor Xa inhibitors.EBI
Corvas International
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.EBI
Glaxosmithkline
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.EBI
Bristol-Myers Squibb
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.EBI
Dupont Pharmaceuticals
Thrombin inhibitors based on [5,5] trans-fused indane lactams.EBI
Glaxo Wellcome Research And Development
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.EBI
Glaxosmithkline R&D
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.EBI
Berlex Biosciences
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.EBI
Dupont Pharmaceuticals
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
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
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.EBI
China Pharmaceutical University
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
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.EBI
The University Of Queensland
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.EBI
Glaxo Wellcome Research And Development
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies.EBI
Dupont Pharmaceuticals
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.EBI
Corvas International
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.EBI
Berlex Biosciences
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.EBI
Berlex Biosciences
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.EBI
3-Dimensional Pharmaceuticals
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 Pharmaceuticals
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.EBI
Bristol-Myers Squibb
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.EBI
Univ. Lille
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.EBI
Philipps University Marburg
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.EBI
Biotech Research Institute
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.EBI
Dupont Pharmaceuticals
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Design of benzamidine-type inhibitors of factor Xa.EBI
Institut FüR Biochemie
Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues.EBI
Universidade Federal De Pernambuco
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
Modulating Heparanase Activity: Tuning Sulfation Pattern and Glycosidic Linkage of Oligosaccharides.EBI
Wayne State University
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.EBI
Collegeville
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.EBI
Dupont Pharmaceuticals
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.EBI
Merck Research Laboratories
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.EBI
The University Of Queensland
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
Discovery of novel, potent, isosteviol-based antithrombotic agents.EBI
Peking University
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
Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.EBI
Corvas International
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.EBI
University Of Antwerp (Ua)
Highly selective tripeptide thrombin inhibitors.EBI
Eli Lilly
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.EBI
Daiichi Pharmaceutical
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI
Thrombosis Research Institute
Three-dimensional quantitative structure-activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices analysis to elucidate selectivity differences of inhibitors binding to trypsin, thrombin, and factor Xa.EBI
University Of Marburg
Semisynthesis of ent-norstrobane diterpenoids as potential inhibitor for factor Xa.EBI
Guangdong-Macau Traditional Chinese Medicine Technology Industrial Park Development
Druggability Assessment of Targets Used in Kinetic Target-Guided Synthesis.EBI
University Of Groningen
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.EBI
University Of Nottingham
Characterizing hydration sites in protein-ligand complexes towards the design of novel ligands.EBI
Sanofi-Aventis Deutschland
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.EBI
Bristol-Myers Squibb
Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity.EBI
German Cancer Research Center (Dkfz)
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.EBI
University Of Wollongong
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.EBI
Hefei University Of Technology
Macrocyclic factor XIa inhibitors.EBI
Bristol-Myers Squibb
Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics.EBI
Virginia Commonwealth University
Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors.EBI
China Pharmaceutical University
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.EBI
Bicycle Therapeutics
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).EBI
Bristol-Myers Squibb
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity.EBI
Shenyang Pharmaceutical University
Neutral macrocyclic factor VIIa inhibitors.EBI
Bristol-Myers Squibb Research And Development
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.EBI
Mochida Pharmaceutical
 
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
8-Carboxamidocyclazocine: a long-acting, novel benzomorphan.BDB
University Of Rochester
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.BDB
Bayer
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.BDB
Vrije Universiteit
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4.BDB
Uppsala University
Fragment-based discovery of novel thymidylate synthase leads by NMR screening and group epitope mapping.BDB
University Of Washington
Synthesis and pharmacological evaluation of analogs of indole-based cannabimimetic agents.BDB
UniversitÀ
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol.BDB
University Of California San Diego
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.BDB
University Of California Berkeley
Picomolar inhibitors as transition-state probes of 5'-methylthioadenosine nucleosidases.BDB
Albert Einstein College Of Medicine
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
ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective PyrazolopyrimidinesBDB
Wyeth Research
5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity.BDB
Wyeth Research
Biarylether amide quinolines as liver X receptor agonists.BDB
Wyeth Research
Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.BDB
Abbott Laboratories
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
Identification of inhibitors of checkpoint kinase 1 through template screening.BDB
The Institute Of Cancer Research
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.BDB
Abbott Laboratories
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.BDB
Abbott Laboratories