55 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Identification of a new series of amides as non-covalent proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Bari &Quot;Aldo Moro&Quot
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Virginia Commonwealth 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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pharmaceutical Research Institute
Identification and prediction of promiscuous aggregating inhibitors among known drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Northwestern University
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Northwestern University
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Gsk
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Welfide
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Horsham Research Centre
Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merrell Dow Research Institute
Design, synthesis, crystal structures, and antimicrobial activity of sulfonamide boronic acids asß-lactamase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of California San Francisco
Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Smithsonian Marine Station At Ft. Pierce
1,3-Oxazino[4,5-b]indole-2,4-(1H,9H)-diones and 5,6-dimethylpyrrolo-[2,3-d]-1,3-oxazin-2,4-(1H,7H)-diones as serine protease inhi...![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Engineering of cyclic peptides with novel inhibiting properties to differentiate two serine proteases, chymotrypsin and subtilisin Carlsberg![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Boric acid effect ont he hydrolysis of 4-nitrophenyl 2,3-dihydroxybenzoate: mimic of borate inhibition of serine proteases![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Borinic acid inhibitors as probes of the factors involved in binding at the active sites of subtilisin carlsberg and α-chymotrypsin![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Senju Pharmaceutical
Alpha-ketoester-based photobiological switches: synthesis, peptide chain extension and assay against alpha-chymotrypsin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Canterbury
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shionogi
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The Oxford Centre For Molecular Sciences
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto Pharmaceutical University
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nippon Steel
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxo Wellcome Research and Development
Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Green Cross Research Laboratories
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Northwestern University Medical School
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxowellcome Medicines Research Centre
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim (Canada)
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Suntory
Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of alpha-chymotrypsin: significance of the"aromatic" nature of the novel ester-type coumarin for strong inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Université
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zeneca Pharmaceuticals
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Thrombosis 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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zeneca Pharmaceuticals
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Csir-National Chemical Laboratory
Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Discovery and validation of 2-styryl substituted benzoxazin-4-ones as a novel scaffold for rhomboid protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Heinrich-Heine University Duesseldorf
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The University of Queensland
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Sharp and Dohme Research Laboratories
O'-(epoxyalkyl)tyrosines and (epoxyalkyl)phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
State University
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Illinois