The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28228366 |
2 |
Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K. |
University Of British Columbia |
27498895 |
6 |
Affinity Crystallography: A New Approach to Extracting High-Affinity Enzyme Inhibitors from Natural Extracts. |
University Of British Columbia |
27214508 |
43 |
Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S. |
Cnrs |
27690432 |
75 |
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). |
Charles River Discovery Research Services |
26985300 |
110 |
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry. |
University Of Bonn |
26280490 |
17 |
Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors. |
National Institute Of Chemistry |
25571794 |
40 |
Structure-based design and optimization of potent inhibitors of the adenoviral protease. |
Novartis Institute For Biomedical Research |
24592859 |
59 |
Cathepsin C inhibitors: property optimization and identification of a clinical candidate. |
Astrazeneca |
23350811 |
57 |
Docking-based virtual screening of covalently binding ligands: an orthogonal lead discovery approach. |
Msd Animal Health Innovation |
24900293 |
78 |
Discovery of novel cyanamide-based inhibitors of cathepsin C. |
TBA |
19962796 |
64 |
3D QSAR studies on ketoamides of human cathepsin K inhibitors based on two different alignment methods. |
Chinese Academy Of Sciences |
19616430 |
120 |
Design of selective Cathepsin inhibitors. |
Astrazeneca |
16546382 |
100 |
Keto-1,3,4-oxadiazoles as cathepsin K inhibitors. |
Celera Genomics |
9804696 |
2 |
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 |
9767629 |
8 |
Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic. |
Smithkline Beecham Pharmaceuticals |
23122525 |
9 |
Fluorescent nitrile-based inhibitors of cysteine cathepsins. |
University Of Bonn |
22984809 |
111 |
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors. |
Astrazeneca |
22742641 |
113 |
(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 |
22686657 |
60 |
Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F. |
University Of Bonn |
22858142 |
121 |
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition. |
Astrazeneca |
21128614 |
76 |
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors. |
University Of Bonn |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University Of Florida |
18375120 |
45 |
New chemotypes for cathepsin K inhibitors. |
Novartis Institutes For Biomedical Research |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
18226527 |
80 |
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
16380250 |
31 |
4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors. |
Sankyo |
15713380 |
16 |
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 |
21733692 |
56 |
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent. |
Glaxosmithkline |
21232956 |
10 |
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
21227690 |
68 |
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 |
21041084 |
102 |
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease. |
Merck Research Laboratories |
21030256 |
61 |
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors. |
Merck Research Laboratories |
20843687 |
60 |
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG. |
Merck Research Laboratories |
19841155 |
29 |
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
Merck Research Laboratories |
20598883 |
83 |
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors. |
Merck Research Laboratories |
20594841 |
123 |
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. |
Merck Research Laboratories |
20580231 |
21 |
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important. |
Merck Research Laboratories |
20218623 |
68 |
Emerging targets in osteoporosis disease modification. |
Amgen |
20153187 |
32 |
Dioxo-triazines as a novel series of cathepsin K inhibitors. |
Schering-Plough |
20149657 |
53 |
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. |
Schering-Plough |
20061146 |
12 |
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor. |
Merck Frosst Centre For Therapeutic Research |
19231183 |
44 |
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors. |
Astrazeneca |
19124252 |
141 |
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 |
19117756 |
27 |
Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors. |
Merck Frosst Centre For Therapeutic Research |
18662880 |
56 |
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors. |
Novartis Institutes For Biomedical Research |
18572405 |
85 |
Discovery of selective and nonpeptidic cathepsin S inhibitors. |
Novartis Institutes For Biomedical Research |
18571402 |
24 |
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 |
18570365 |
29 |
The many roles for fluorine in medicinal chemistry. |
Merck Research Laboratories |
18313933 |
18 |
Substrate optimization for monitoring cathepsin C activity in live cells. |
Genomics Institute Of The Novartis Research Foundation |
11975521 |
2 |
Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K. |
Millennium Pharmaceuticals |
11975520 |
3 |
A new dimeric dihydrochalcone and a new prenylated flavone from the bud covers of Artocarpus altilis: potent inhibitors of cathepsin K. |
Millennium Pharmaceuticals |
17911019 |
50 |
Novel scaffold for cathepsin K inhibitors. |
Novartis Institutes For Biomedical Research |
17544269 |
30 |
Primary amides as selective inhibitors of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
17196818 |
90 |
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases. |
The Genomics Institute Of The Novartis Research Foundation |
16750630 |
28 |
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K. |
Celera Genomics |
16376075 |
28 |
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors. |
Glaxosmithkline |
16290936 |
69 |
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? |
Glaxosmithkline |
16250645 |
35 |
Azepanone-based inhibitors of human cathepsin L. |
Glaxosmithkline |
16154747 |
37 |
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K. |
Merck Frosst Centre For Therapeutic Research |
15993587 |
11 |
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles. |
Glaxosmithkline |
15982880 |
86 |
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
15896958 |
32 |
Acyclic cyanamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
15837295 |
55 |
A structural screening approach to ketoamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
15780613 |
28 |
Novel and potent cyclic cyanamide-based cathepsin K inhibitors. |
Glaxosmithkline |
15537340 |
27 |
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K. |
Novartis Institutes For Biomedical Research |
15456249 |
22 |
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications. |
Glaxosmithkline |
15456248 |
33 |
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K. |
Glaxosmithkline |
15341947 |
57 |
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions. |
Glaxosmithkline |
15261289 |
38 |
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors. |
Merck Frosst Centre For Therapeutic Research |
15177446 |
41 |
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors. |
Glaxosmithkline |
15109647 |
11 |
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
14741275 |
27 |
Design of small molecule ketoamide-based inhibitors of cathepsin K. |
Glaxosmithkline |
14736240 |
57 |
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k. |
Glaxosmithkline |
14684342 |
39 |
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors. |
Glaxosmithkline |
14684338 |
44 |
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors. |
Eli Lilly |
14684304 |
41 |
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors. |
Amgen |
12781193 |
36 |
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity. |
Ligand Pharmaceuticals |
12781182 |
81 |
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents. |
Novartis Pharma |
12467634 |
67 |
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors. |
Currently Naeja Pharmaceutical |
12431059 |
27 |
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides. |
National Research Council Of Canada |
12419374 |
45 |
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S. |
Currently Naeja Pharmaceutical |
12419373 |
18 |
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 |
12270191 |
36 |
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain. |
University Of California |
12270170 |
42 |
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors. |
Celera |
12213061 |
23 |
Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. |
University Of Gda£?Sk |
12036343 |
24 |
Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors. |
TBA |
11677133 |
14 |
Discovery and parallel synthesis of a new class of cathepsin K inhibitors. |
Bayer Research Center |
11311061 |
40 |
Azepanone-based inhibitors of human and rat cathepsin K. |
Glaxosmithkline |
11206458 |
14 |
Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K. |
Smithkline Beecham Pharmaceuticals |
11206457 |
29 |
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K. |
Smithkline Beecham Pharmaceuticals |
11141092 |
85 |
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L. |
Merck Frosst Centre For Therapeutic Research |
10450951 |
3 |
Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K. |
Smithkline Beecham Pharmaceuticals |
9733481 |
31 |
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K. |
Smithkline Beecham Pharmaceuticals |
7650671 |
15 |
Vinyl sulfones as mechanism-based cysteine protease inhibitors. |
Khepri Pharmaceuticals |
23356427 |
16 |
Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide. |
Sakarya University |
21635213 |
8 |
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II. |
Balikesir University |
10455251 |
10 |
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. |
Roche Bioscience |
1397049 |
24 |
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists. |
Novo Nordisk |
15734651 |
135 |
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists. |
National Institutes Of Health |
19620011 |
80 |
Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy. |
Universita Degli Studi Di Milano |
15225699 |
27 |
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors. |
Eli Lilly |