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

58 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).EBI
Charles River Discovery Research Services
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.EBI
Boehringer Ingelheim (Canada)
Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.EBI
Chang Gung University
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.EBI
Hokkaido University
Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.EBI
Universidade De Lisboa
Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design.EBI
Asubio Pharma
Discovery of potent, selective chymase inhibitors via fragment linking strategies.EBI
Boehringer Ingelheim Pharmaceuticals
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.EBI
Celera Genomics
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.EBI
Aarhus University
N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.EBI
University Of Lisbon
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.EBI
Federal University Of Alfenas
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.EBI
Merck Research Laboratories
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.EBI
Cephalon
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).EBI
Gsk
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase.EBI
Welfide
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.EBI
Welfide
Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.EBI
Georgia Institute Of Technology
Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.EBI
Boehringer Ingelheim Pharmaceuticals
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.EBI
Aristotle University Of Thessaloniki
Phage-encoded combinatorial chemical libraries based on bicyclic peptides.EBI
Laboratory Of Molecular Biology, Medical Research Council
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
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.EBI
Merck Frosst Canada
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.EBI
National Human Genome Research Institute
 
Janus compounds: dual inhibitors of proteinasesEBI
TBA
Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors.EBI
University Of Gda£?Sk
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.EBI
University Of Leipzig
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.EBI
Daiichi Asubio Pharma
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.EBI
Daiichi Asubio Pharma
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.EBI
Johnson & Johnson Pharmaceutical Research And Development
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.EBI
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.EBI
Toa Eiyo
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.EBI
Shionogi
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.EBI
Shionogi
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.EBI
Shionogi
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.EBI
Roche Pharma Research And Early Development
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.EBI
Kyoto Pharmaceutical University
Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.EBI
Nippon Steel
Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.EBI
The University Of Queensland
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
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.EBI
The University Of Queensland
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.EBI
Proscript
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.EBI
Glaxowellcome Medicines Research Centre
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.EBI
Zeneca Pharmaceuticals
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.EBI
RhôNe-Poulenc Rorer
Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective.EBI
Indian Institute Of Technology (Bhu)
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.EBI
Suntory
Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.EBI
The University Of Queensland
Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.EBI
Zeneca Pharmaceuticals
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.EBI
Thrombosis Research Institute
New orally active serine protease inhibitors.EBI
Minase Research Institute
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.EBI
Zeneca Pharmaceuticals
On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients.EBI
Virginia Commonwealth University
Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G.EBI
Merrell Dow Research Institute
Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold.EBI
The University Of Queensland
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.EBI
Bicycle Therapeutics
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.BDB
Parke-Davis Pharmaceutical Research