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159 articles for thisTarget


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

PMID
Data
Article Title
Organization
Prospective Evaluation of Free Energy Calculations for the Prioritization of Cathepsin L Inhibitors.EBI
Roche Pharmaceutical Research And Early Development (Pred)
Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.EBI
Baylor University
Evaluation of dipeptide nitriles as inhibitors of rhodesain, a major cysteine protease of Trypanosoma brucei.EBI
Johannes Gutenberg University
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.EBI
Universitat Jaume I
Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.EBI
Cnrs
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).EBI
Charles River Discovery Research Services
De Novo Design at the Edge of Chaos.EBI
Swiss Federal Institute Of Technology (Eth)
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
Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.EBI
National Institute Of Chemistry
Structure-based design and optimization of potent inhibitors of the adenoviral protease.EBI
Novartis Institute For Biomedical Research
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.EBI
Universidade Federal De S£O Carlos
Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.EBI
Eli Lilly
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.EBI
University Of Bonn
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.EBI
Astrazeneca
Principles and applications of halogen bonding in medicinal chemistry and chemical biology.EBI
Eberhard-Karls 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
Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.EBI
Boehringer Ingelheim Pharmaceuticals
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.EBI
Universidade Federal De Pernambuco
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
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
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and V.EBI
Universidade Federal De S£O Carlos
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£
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
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.EBI
University Of Pennsylvania
New chemotypes for cathepsin K inhibitors.EBI
Novartis Institutes For Biomedical Research
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.EBI
University Of Pennsylvania
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI
Johnson & Johnson Pharmaceutical Research & Development
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
Designed multiple ligands. An emerging drug discovery paradigm.EBI
Organon Laboratories
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
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.EBI
University Of Messina
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.EBI
Glaxosmithkline
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
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
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
 
Inhibition of human erythrocyte calpain I by novel quinolinecarboxamidesEBI
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
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity.EBI
Medivir
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.EBI
Novartis Institutes For Biomedical Research
Effect of cathepsin K inhibitors on bone resorption.EBI
Novartis Institutes For Biomedical Research
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.EBI
University Of Leipzig
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.EBI
Novartis Institutes For Biomedical Research
Discovery of selective and nonpeptidic cathepsin S inhibitors.EBI
Novartis Institutes For Biomedical Research
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
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 and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.EBI
Celera Genomics
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.EBI
Arpida
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
Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.EBI
University Of WüRzburg
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
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.EBI
Novartis Institutes For Biomedical Research
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
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.EBI
Novartis Pharma
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.EBI
Currently Naeja Pharmaceutical
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.EBI
National Research Council Of Canada
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
Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.EBI
TBA
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.EBI
Abbott
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin.EBI
Organon K.K.
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
Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.EBI
Queen'S University Belfast
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.EBI
Smithkline Beecham Pharmaceuticals
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.EBI
University Of California
Chalcones, inhibitors for topoisomerase I and cathepsin B and L, as potential anti-cancer agents.EBI
Cha University
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?EBI
National Institute Of Biology
Small-molecule inhibitors of cathepsin L incorporating functionalized ring-fused molecular frameworks.EBI
Baylor University
Vinyl sulfones as mechanism-based cysteine protease inhibitors.EBI
Khepri Pharmaceuticals
New aziridine-based inhibitors of cathepsin L-like cysteine proteases with selectivity for the Leishmania cysteine protease LmCPB2.8.EBI
Johannes Gutenberg-Universit£T Mainz
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.EBI
Cnrs Upr 4301
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.EBI
Universit£
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates.EBI
Universitat Jaume I
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.EBI
Irbm Science Park
Cathepsin B inhibitors: Further exploration of the nitroxoline core.EBI
University Of Ljubljana
Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.EBI
University Of Michigan
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.EBI
Eth Zurich
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.EBI
Eth Zurich
Asymmetric synthesis and evaluation of epoxy-?-acyloxycarboxamides as selective inhibitors of cathepsin L.EBI
Federal University Of S£O Carlos
Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).EBI
University Of Messina
Synthesis of a-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase.BDB
Institute For Advanced Studies In Basic Sciences (Iasbs)
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.BDB
Balikesir University
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.BDB
Novo Nordisk
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.BDB
National Institutes Of Health