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156 articles for thisTarget


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

PMID
Data
Article Title
Organization
Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.EBI
Whitman College
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.EBI
University Of Bonn
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.EBI
Baylor University
Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.EBI
Hebei University Of Science & Technology
SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.EBI
Kurukshetra University
Structure-based design and optimization of potent inhibitors of the adenoviral protease.EBI
Novartis Institute For Biomedical Research
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.EBI
Array Biopharma
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.EBI
Universidade Federal De S£O Carlos
The discovery of potent, selective, and reversible inhibitors of the house dust mite peptidase allergen Der p 1: an innovative approach to the treatment of allergic asthma.EBI
Domainex
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.EBI
University Of Bonn
Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors.EBI
E£Tv£S Lor£Nd University (Elte)
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.EBI
Astrazeneca
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.EBI
Hokkaido University
Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.EBI
Kurukshetra University
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.EBI
University Of Ljubljana
Discovery of novel cyanamide-based inhibitors of cathepsin C.EBI
TBA
Design of selective Cathepsin inhibitors.EBI
Astrazeneca
Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.EBI
Celera Genomics
Fluorescent nitrile-based inhibitors of cysteine cathepsins.EBI
University Of Bonn
Synopsis of some recent tactical application of bioisosteres in drug design.EBI
Bristol-Myers Squibb Pharmaceutical Research And Development
Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases.EBI
TBA
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.EBI
Astrazeneca
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.EBI
Astrazeneca
Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.EBI
University Of Bonn
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.EBI
Hokkaido University
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.EBI
Astrazeneca
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.EBI
TBA
Exploring activity cliffs in medicinal chemistry.EBI
Rheinische Friedrich-Wilhelms-Universit£T
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.EBI
University Of Bonn
Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.EBI
Universit£
Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.EBI
Universit£
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI
University Of Florida
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.EBI
Federal University Of Alfenas
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.EBI
Ewha Womans University
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 trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.EBI
University Of California
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI
Johnson & Johnson Pharmaceutical Research & Development
Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain.EBI
Pukyong National University
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.EBI
University Of Messina
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.EBI
Merck Frosst Centre For Therapeutic Research
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.EBI
Santhera Pharmaceuticals
Protease inhibitors: current status and future prospects.EBI
University Of Queensland
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.EBI
Takeda Chemical Industries
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.EBI
Cephalon
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.EBI
Maxim Pharmaceuticals
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.EBI
Boehringer Ingelheim Pharmaceuticals
 
Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin LEBI
TBA
Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors.EBI
National Chemical Laboratory (Csir-Ncl)
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.EBI
University Of Messina
Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B.EBI
University Of Ljubljana
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.EBI
Boehringer Ingelheim (Canada)
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.EBI
Merck Research Laboratories
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.EBI
Merck Research Laboratories
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.EBI
Merck Research Laboratories
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.EBI
Baylor University
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.EBI
Merck Research Laboratories
Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.EBI
Georgia Institute Of Technology
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.EBI
Merck Research Laboratories
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.EBI
University Of WüRzburg
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.EBI
Merck Research Laboratories
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.EBI
University Of Duisburg-Essen
Dioxo-triazines as a novel series of cathepsin K inhibitors.EBI
Schering-Plough
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.EBI
Schering-Plough
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.EBI
Merck Frosst Canada
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.EBI
Baylor University
Structure-guided development of selective TbcatB inhibitors.EBI
University Of California
 
Nonpeptidic inhibitors of recombinant human calpain IEBI
TBA
 
Oligopresentation of protease inhibitors with β-cyclodextrin as templateEBI
TBA
 
Inhibition of human erythrocyte calpain I by novel quinolinecarboxamidesEBI
TBA
 
Design of a new selective cysteine protease inactivator and its mechanistic implicationsEBI
TBA
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.EBI
University Of Messina
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.EBI
Astrazeneca
Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.EBI
University Of Toyama
Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.EBI
Bar-Ilan University
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.EBI
The University Of Tennessee Health Science Center
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.EBI
Korea Research Institute Of Chemical Technology
Substrate optimization for monitoring cathepsin C activity in live cells.EBI
Genomics Institute Of The Novartis Research Foundation
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.EBI
LinköPing University
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.EBI
University Of Pennsylvania
Primary amides as selective inhibitors of cathepsin K.EBI
Merck Frosst Centre For Therapeutic Research
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.EBI
The Genomics Institute Of The Novartis Research Foundation
Design of potent inhibitors of human beta-secretase. Part 2.EBI
Pfizer
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.EBI
The University Of Tennessee Health Science Center
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.EBI
Celera Genomics
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.EBI
Celera
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.EBI
Arpida
A novel series of urea-based peptidomimetic calpain inhibitors.EBI
The University Of Tennessee Health Science Center
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.EBI
Celera Genomics
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?EBI
Glaxosmithkline
Azepanone-based inhibitors of human cathepsin L.EBI
Glaxosmithkline
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.EBI
Merck Frosst Centre For Therapeutic Research
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
Acyclic cyanamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
A structural screening approach to ketoamide-based inhibitors of cathepsin K.EBI
Glaxosmithkline
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.EBI
Glaxosmithkline
Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.EBI
Université
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.EBI
Boehringer Ingelheim (Canada)
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).EBI
University Of Southern California
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.EBI
Eli Lilly
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.EBI
Glaxosmithkline
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.EBI
Merck Frosst Centre For Therapeutic Research
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.EBI
Glaxosmithkline
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.EBI
Eli Lilly
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.EBI
Amgen
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.EBI
Novartis Institute Of Biomedical Research
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.EBI
Ligand Pharmaceuticals
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.EBI
Abbott
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.EBI
University Of Tennessee Health Science Center
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI
Senju Pharmaceutical
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.EBI
National Research Council Of Canada
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.EBI
Currently Naeja Pharmaceutical
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.EBI
Currently Naeja Pharmaceutical
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.EBI
University Of California
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.EBI
Celera
Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.EBI
University Of Gda£?Sk
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.EBI
Abbott
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.EBI
University Of California
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.EBI
Novartis Pharmaceuticals
Potent reversible inhibitors of the protein tyrosine phosphatase CD45.EBI
Astrazeneca Pharmaceuticals
Azepanone-based inhibitors of human and rat cathepsin K.EBI
Glaxosmithkline
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.EBI
Merck Frosst Centre For Therapeutic Research
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.EBI
The University Of Tennessee Health Science Center
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.EBI
Knoll
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.EBI
Brown University
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.EBI
Boehringer Ingelheim (Canada)
P2-proline-derived inhibitors of calpain I.EBI
Cephalon
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.EBI
Boehringer Ingelheim (Canada)
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.EBI
Proscript
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.EBI
Smithkline Beecham Pharmaceuticals
Peptidomimetic inhibitors of the human cytomegalovirus protease.EBI
Boehringer Ingelheim
Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.EBI
Georgia Institute Of Technology
Vinyl sulfones as mechanism-based cysteine protease inhibitors.EBI
Khepri Pharmaceuticals
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.BDB
Balikesir University
 
Design, synthesis and evaluation of trisubstituted thiazoles targeting plasmodium falciparum cysteine proteasesBDB
University, Mississippi
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.BDB
Abbott Laboratories
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.BDB
Abbott Laboratories
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.BDB
Roche Bioscience