150 articles for thisTarget

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

PMID	Data	Article Title	Organization
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
25313327	11	Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.	Eli Lilly
25313316	20	3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.	University of Bonn
24592859	59	Cathepsin C inhibitors: property optimization and identification of a clinical candidate.	Astrazeneca
23313244	57	Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.	Janssen Research and Development
24900293	78	Discovery of novel cyanamide-based inhibitors of cathepsin C.	TBA
19616430	120	Design of selective Cathepsin inhibitors.	Astrazeneca
16546382	100	Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.	Celera Genomics
23122525	9	Fluorescent nitrile-based inhibitors of cysteine cathepsins.	University of Bonn
23084902	116	Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.	Boehringer Ingelheim Pharmaceuticals
21413808	170	Synopsis of some recent tactical application of bioisosteres in drug design.	Bristol-Myers Squibb Pharmaceutical Research and Development
23167554	28	Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.	Universidade Federal De Pernambuco
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
20541404	12	Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
19715320	87	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.	University of Florida
17535802	91	Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.	Merck Research Laboratories
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
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
12036355	36	Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.	University of Parma
21733692	56	Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.	Glaxosmithkline
19171797	1	In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor.	Tibotec
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
20804202	1	Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.	Duquesne University
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
20481438	33	Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.	National Tsing Hua University
20188543	65	Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors.	Johnson & Johnson Pharmaceutical Research & Development
20171097	54	Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions.	Johnson & Johnson Pharmaceutical Research & Development
20153648	47	Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.	Johnson & Johnson Pharmaceutical Research & Development
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
20102207	7	Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.	China Medical University
19665376	48	Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.	Merck Frosst Canada
19783435	50	Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency.	Johnson & Johnson Pharmaceutical Research and Development
	12	MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.	TBA
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
18783943	35	Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.	Novartis Institutes For Biomedical Research
18707091	14	Effect of cathepsin K inhibitors on bone resorption.	Novartis Institutes For Biomedical 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
18313933	18	Substrate optimization for monitoring cathepsin C activity in live cells.	Genomics Institute of The Novartis Research Foundation
17911019	50	Novel scaffold for cathepsin K inhibitors.	Novartis Institutes For Biomedical Research
17822900	48	Pyrazole-based cathepsin S inhibitors with improved cellular potency.	Johnson & Johnson Pharmaceutical Research & Development
17544269	30	Primary amides as selective inhibitors of cathepsin K.	Merck Frosst Centre For Therapeutic Research
17379516	44	Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.	Boehringer Ingelheim Pharmaceuticals
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
16686537	165	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.	Celera
16458510	59	The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors.	Johnson and Johnson Pharmaceutical Research and Development
16302794	53	Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.	Celera Genomics
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
15982880	86	P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.	Glaxosmithkline
15837295	55	A structural screening approach to ketoamide-based inhibitors of cathepsin K.	Glaxosmithkline
15745822	43	Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.	Johnson and Johnson Pharmaceutical Research and Development
15537340	27	Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.	Novartis Institutes For Biomedical Research
15369380	10	Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.	Johnson & Johnson Pharmaceutical Research and Development
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
14592520	41	N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.	Novartis Institute of Biomedical Research
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
12459015	68	Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors.	Boehringer Ingelheim Pharmaceuticals
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
12270170	42	Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.	Celera
12036343	24	Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.	TBA
11741472	45	Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.	Novartis Pharmaceuticals
11356112	175	Potent reversible inhibitors of the protein tyrosine phosphatase CD45.	Astrazeneca Pharmaceuticals
11311061	40	Azepanone-based inhibitors of human and rat cathepsin K.	Glaxosmithkline
31145622	91	Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.	National Institute of Biological Sciences (Nibs)
30773420	16	Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.	Jilin University
32125159	60	Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.	Texas A&M University
26522952	44	Development of a potent and selective cell penetrant Legumain inhibitor.	Queen'S University Belfast
23562595	98	Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?	National Institute of Biology
7650671	15	Vinyl sulfones as mechanism-based cysteine protease inhibitors.	Khepri Pharmaceuticals
29272750	15	Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.	Cnrs Upr 4301
30049585	73	Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.	Universit£
29615344	101	Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.	Irbm Science Park
29590750	58	Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.	Eth Zurich
28759231	46	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
28820254	17	Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.	Emory Chemical Biology Discovery Center Emory University School of Medicine Atlanta
22397393	5	Synthesis of a-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase.	Institute For Advanced Studies In Basic Sciences (Iasbs)
21635213	8	In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.	Balikesir University
11160626	23	In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.	Japan Tobacco
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
19006379	6	Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors.	University of Ferrara