PMID

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Article Title

Organization

Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K.

University Of British Columbia

Affinity Crystallography: A New Approach to Extracting High-Affinity Enzyme Inhibitors from Natural Extracts.

University Of British Columbia

Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.

Cnrs

Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).

Charles River Discovery Research Services

Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.

University Of Bonn

Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.

National Institute Of Chemistry

Structure-based design and optimization of potent inhibitors of the adenoviral protease.

Novartis Institute For Biomedical Research

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.

Astrazeneca

Docking-based virtual screening of covalently binding ligands: an orthogonal lead discovery approach.

Msd Animal Health Innovation

Discovery of novel cyanamide-based inhibitors of cathepsin C.

TBA

3D QSAR studies on ketoamides of human cathepsin K inhibitors based on two different alignment methods.

Chinese Academy Of Sciences

Design of selective Cathepsin inhibitors.

Astrazeneca

Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.

Celera Genomics

Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.

Smithkline Beecham Pharmaceuticals

Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.

Smithkline Beecham Pharmaceuticals

Fluorescent nitrile-based inhibitors of cysteine cathepsins.

University Of Bonn

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.

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.

Astrazeneca

Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.

University Of Bonn

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.

Astrazeneca

Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.

University Of Bonn

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University Of Florida

New chemotypes for cathepsin K inhibitors.

Novartis Institutes For Biomedical Research

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Johnson & Johnson Pharmaceutical Research & Development

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

Merck Frosst Centre For Therapeutic Research

4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors.

Sankyo

cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.

Amura Therapeutics

Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.

Glaxosmithkline

Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

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.

Merck Research Laboratories

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.

Merck Research Laboratories

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.

Merck Research Laboratories

Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.

Merck Research Laboratories

MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.

Merck Research Laboratories

6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.

Merck Research Laboratories

2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.

Merck Research Laboratories

4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.

Merck Research Laboratories

Emerging targets in osteoporosis disease modification.

Amgen

Dioxo-triazines as a novel series of cathepsin K inhibitors.

Schering-Plough

Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.

Schering-Plough

The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.

Merck Frosst Centre For Therapeutic Research

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.

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.

Medivir

Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors.

Merck Frosst Centre For Therapeutic Research

4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.

Novartis Institutes For Biomedical Research

Discovery of selective and nonpeptidic cathepsin S inhibitors.

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.

Korea Research Institute Of Chemical Technology

The many roles for fluorine in medicinal chemistry.

Merck Research Laboratories

Substrate optimization for monitoring cathepsin C activity in live cells.

Genomics Institute Of The Novartis Research Foundation

Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K.

Millennium Pharmaceuticals

A new dimeric dihydrochalcone and a new prenylated flavone from the bud covers of Artocarpus altilis: potent inhibitors of cathepsin K.

Millennium Pharmaceuticals

Novel scaffold for cathepsin K inhibitors.

Novartis Institutes For Biomedical Research

Primary amides as selective inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.

The Genomics Institute Of The Novartis Research Foundation

Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.

Celera Genomics

Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.

Glaxosmithkline

Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

Glaxosmithkline

Azepanone-based inhibitors of human cathepsin L.

Glaxosmithkline

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.

Glaxosmithkline

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

Acyclic cyanamide-based inhibitors of cathepsin K.

Glaxosmithkline

A structural screening approach to ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

Novel and potent cyclic cyanamide-based cathepsin K inhibitors.

Glaxosmithkline

Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.

Novartis Institutes For Biomedical Research

Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.

Glaxosmithkline

Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.

Glaxosmithkline

Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.

Glaxosmithkline

Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.

Merck Frosst Centre For Therapeutic Research

Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.

Glaxosmithkline

Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

Design of small molecule ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.

Glaxosmithkline

Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.

Glaxosmithkline

P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.

Eli Lilly

(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.

Amgen

3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.

Ligand Pharmaceuticals

Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.

Novartis Pharma

3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.

Currently Naeja Pharmaceutical

Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.

National Research Council Of Canada

6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.

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.

Currently Naeja Pharmaceutical

General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.

University Of California

Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.

Celera

Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.

University Of Gda£?Sk

Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.

TBA

Discovery and parallel synthesis of a new class of cathepsin K inhibitors.

Bayer Research Center

Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors.

Federal University Of S£O Carlos

Azepanone-based inhibitors of human and rat cathepsin K.

Glaxosmithkline

Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K.

Smithkline Beecham Pharmaceuticals

Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.

Smithkline Beecham Pharmaceuticals

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

Merck Frosst Centre For Therapeutic Research

Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors.

Northeastern University

Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.

Shanghai Jiao-Tong University School Of Medicine

Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.

Smithkline Beecham Pharmaceuticals

Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.

Jilin University

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.

Smithkline Beecham Pharmaceuticals

Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?

National Institute Of Biology

Vinyl sulfones as mechanism-based cysteine protease inhibitors.

Khepri Pharmaceuticals

Natural inhibitors targeting osteoclast-mediated bone resorption.

Chinese Academy Of Sciences

Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.

Cnrs Upr 4301

Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.

Universit£

Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.

Irbm Science Park

Asymmetric synthesis and evaluation of epoxy-?-acyloxycarboxamides as selective inhibitors of cathepsin L.

Federal University Of S£O Carlos

Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.

Novartis Institutes For Biomedical Research

Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer's Disease: 2-(3-Phenyl-1H-pyrazol-1-yl)-nicotinamides.

Abbvie Deutschland

Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide.

Sakarya University

In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.

Balikesir University

RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Roche Bioscience

NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.

Novo Nordisk

A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.

National Institutes Of Health

Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.

Universita Degli Studi Di Milano

Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.

Eli Lilly