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50 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
Universit£
Identification of a new series of amides as non-covalent proteasome inhibitors.EBI
Universit£
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
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.EBI
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
Pharmaceutical Research Institute
Identification and prediction of promiscuous aggregating inhibitors among known drugs.EBI
Northwestern University
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.EBI
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
Gsk
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.EBI
Welfide
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.EBI
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
Merrell Dow Research Institute
 
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitorEBI
TBA
Proteasome inhibitors for cancer therapy.EBI
Cephalon
Design, synthesis, crystal structures, and antimicrobial activity of sulfonamide boronic acids asß-lactamase inhibitors.EBI
University Of California San Francisco
Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis.EBI
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
TBA
 
Diphenylborinic acid is a strong inhibitor of serine proteasesEBI
TBA
 
Stereochemical approach for enzyme inhibitor designEBI
TBA
 
Engineering of cyclic peptides with novel inhibiting properties to differentiate two serine proteases, chymotrypsin and subtilisin CarlsbergEBI
TBA
 
Boric acid effect ont he hydrolysis of 4-nitrophenyl 2,3-dihydroxybenzoate: mimic of borate inhibition of serine proteasesEBI
TBA
 
Janus compounds: dual inhibitors of proteinasesEBI
TBA
 
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.EBI
TBA
 
Borinic acid inhibitors as probes of the factors involved in binding at the active sites of subtilisin carlsberg and α-chymotrypsinEBI
TBA
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.EBI
Eli Lilly
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI
Senju Pharmaceutical
Alpha-ketoester-based photobiological switches: synthesis, peptide chain extension and assay against alpha-chymotrypsin.EBI
University Of Canterbury
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.EBI
Shionogi
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.EBI
The Oxford Centre For Molecular Sciences
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.EBI
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
Nippon Steel
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.EBI
Glaxo Wellcome Research And Development
Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.EBI
Green Cross Research Laboratories
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.EBI
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
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
Merck Research Laboratories
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.EBI
Boehringer Ingelheim (Canada)
Peptidomimetic inhibitors of the human cytomegalovirus protease.EBI
Boehringer Ingelheim
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.EBI
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
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
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
Carboxyl-modified amino acids and peptides as protease inhibitors.EBI
TBA
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.EBI
Merck Sharp And Dohme Research Laboratories
O'-(epoxyalkyl)tyrosines and (epoxyalkyl)phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism.EBI
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
University Of Illinois
Design and characterization of bivalent BET inhibitors.BDB
Dana-Farber Cancer Institute
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.BDB
Centre De Recherches De Croissy