120 articles for thisTarget
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Article Title
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Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Novartis Pharma
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.
Bristol-Myers Squibb
Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity.
Ecole Polytechnique F�D�Rale De Lausanne (Epfl)
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors.
Global Blood Therapeutics
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.
Bristol-Myers Squibb R & D
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.
Bristol-Myers Squibb R & D
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Bristol-Myers Squibb
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Bristol-Myers Squibb
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.
Bristol-Myers Squibb
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
Bristol-Myers Squibb
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.
Bristol-Myers Squibb
Inhibitors of Factor XIa and Plasma Kallikrein May Treat Thromboembolic Disorders and Many Diabetes Complications.
Therachem Research Medilab (India)
Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.
TBA
Pyrrolopyrimidine-inhibitors with hydantoin moiety as spacer can explore P4/S4 interaction on plasmin.
Hiroshima International University
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.
Ecole Polytechnique F�D�Rale De Lausanne Epfl
Development of new cyclic plasmin inhibitors with excellent potency and selectivity.
Philipps University Marburg
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Celera Genomics
A new strategy for the development of highly potent and selective plasmin inhibitors.
Philipps University Marburg
Human kallikrein 6 inhibitors with a para-amidobenzylanmine P1 group identified through virtual screening.
Sanofi Pharmaceuticals
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University Of Florida
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Bristol-Myers Squibb Research And Development
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
Bristol-Myers Squibb
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library.
Brown University
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).
Pharmaceutical Research Institute
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.
Dupont Pharmaceuticals
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Merck Research Laboratories
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.
Klinikum Der Friedrich-Schiller-Universit£T Jena
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.
University Of Arkansas
Synthesis of potent and selective inhibitors of human plasma kallikrein.
The Procter & Gamble
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors.
Universit£T Bielefeld
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.
Astellas Pharma
Identification of novel plasmin inhibitors possessing nitrile moiety as warhead.
Hiroshima International University
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.
Philipps University Marburg
Phage-encoded combinatorial chemical libraries based on bicyclic peptides.
Laboratory Of Molecular Biology, Medical Research Council
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications.
Bristol-Myers Squibb
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Glaxosmithkline
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Celera Genomics
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
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.
Abbott Laboratories
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Novartis Institutes For Biomedical Research
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Substrate-Guided Design of Selective FXIIa Inhibitors Based on the Plant-Derived Momordica cochinchinensis Trypsin Inhibitor-II (MCoTI-II) Scaffold.
The University Of Queensland
Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.
Philipps University Marburg
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.
Chinese Academy Of Sciences
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.
University Of Wollongong
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Glaxosmithkline
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.
Glaxosmithkline R&D
New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm.
Astrazeneca
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.
The University Of Queensland
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.
Philipps University Marburg
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Merck Research Laboratories
Potent, Selective, and Cell-Penetrating Inhibitors of Kallikrein-Related Peptidase 4 Based on the Cyclic Peptide MCoTI-II.
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.
Merck Research Laboratories
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.
University Of Antwerp (Ua)
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.
Aarhus University
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.
University Of Nottingham
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.
Bristol-Myers Squibb
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
University Of Wollongong
Plasma Kallikrein Inhibitors for the Treatment of Retinal Vascular Permeability Associated with Diabetic Retinopathy and Diabetic Macular Edema.
Therachem Research Medilab (India)
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Bicycle Therapeutics
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Bristol-Myers Squibb
Neutral macrocyclic factor VIIa inhibitors.
Bristol-Myers Squibb Research And Development
Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles
Hacettepe University
Molecular and pharmacological characterization of native cortical gamma-aminobutyric acidA receptors containing both alpha1 and alpha3 subunits.
Universidad De Sevilla
Development and biological evaluation of a novel aurora A kinase inhibitor.
Parc De Recerca Biomedica De Barcelona
A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides.
University Of Toronto
Activity-based probes that target diverse cysteine protease families.
Stanford University
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University Of Cambridge
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.
Northern Kentucky University
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.
Pfizer
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.
University Of Tokyo
3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.
Abbott Laboratories
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
Vernalis (R&D)
Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors.
Universita Di Napoli Federico Ii
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
Parke-Davis Pharmaceutical Research
Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors.
Durham University