240 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.
Baylor University
Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.
The University of Tokyo
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.
Universitat Jaume I
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
Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.
Whitman College
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.
University of Bonn
Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease.
Yamagata University
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.
Baylor University
Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.
Hebei University of Science & Technology
Lower homologues of ahpatinin, aspartic protease inhibitors, from a marine Streptomyces sp.
The University of Tokyo
SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.
Kurukshetra University
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Novartis Institute For Biomedical Research
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
Array Biopharma
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.
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.
Domainex
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.
University of Bonn
Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors.
E£Tv£S Lor£Nd University (Elte)
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
Astrazeneca
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.
Hokkaido University
Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.
Kurukshetra University
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.
University of Ljubljana
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases.
TBA
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
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.
Hokkaido University
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Astrazeneca
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.
TBA
Exploring activity cliffs in medicinal chemistry.
Rheinische Friedrich-Wilhelms-Universit£T
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.
University of Bonn
Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.
University of Messina
Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.
University of Messina
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.
Federal University of Alfenas
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
Ewha Womans University
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Merck Research Laboratories
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
University of California
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain.
Pukyong National University
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.
University of Messina
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.
Santhera Pharmaceuticals
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.
Takeda Chemical Industries
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
Cephalon
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.
University of Arkansas
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Maxim Pharmaceuticals
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.
Boehringer Ingelheim Pharmaceuticals
Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain.
Hoechst Marion Roussel
Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors.
National Chemical Laboratory (Csir-Ncl)
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.
University of Messina
Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B.
University of Ljubljana
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
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.
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
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
Baylor University
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Merck Research Laboratories
Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.
Georgia Institute of Technology
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Merck Research Laboratories
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.
University of WüRzburg
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Merck Research Laboratories
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
University of Duisburg-Essen
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Schering-Plough
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
Merck Frosst Canada
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
Baylor University
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
University of Messina
Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.
University of Toyama
Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.
Bar-Ilan University
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.
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.
Korea Research Institute of Chemical Technology
Substrate optimization for monitoring cathepsin C activity in live cells.
Genomics Institute of The Novartis Research Foundation
Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.
University of ZüRich
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.
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.
University of Pennsylvania
Primary amides as selective inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Discovery, synthesis and mechanism study of 2,3,5-substituted [1,2,4]-thiadiazoles as covalent inhibitors targeting 3C-Like protease of SARS-CoV-2.
Shanghaitech University
Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.
Whitman College
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
Calibr At Scripps Research Institute
Discovery of quinazolin-4-one-based non-covalent inhibitors targeting the severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2 M
China Pharmaceutical University
Structure-based lead optimization of peptide-based vinyl methyl ketones as SARS-CoV-2 main protease inhibitors.
University of Messina
Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2) and middle east respiratory syndrome coronavirus (MERS-CoV).
Wichita State University
Falcipains: Biochemistry, target validation and structure-activity relationship studies of inhibitors as antimalarials.
University of Petroleum and Energy Studies
Discovery and Mechanism Study of SARS-CoV-2 3C-like Protease Inhibitors with a New Reactive Group.
Shanghaitech University
Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.
Helmholtz-Zentrum Dresden-Rossendorf
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
The Genomics Institute of The Novartis Research Foundation
Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells.
Shenyang Pharmaceutical University
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.
The University of Tennessee Health Science Center
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.
China Pharmaceutical University
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Celera Genomics
Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.
Anhui Medical University
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
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.
Shionogi
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
The University of Sydney
Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2.
China Pharmaceutical University
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Shandong University
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
Niddk
A novel series of urea-based peptidomimetic calpain inhibitors.
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.
Celera Genomics
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Glaxosmithkline
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.
University of Alberta Edmonton
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
New peptidomimetic rhodesain inhibitors with improved selectivity towards human cathepsins.
Johannes Gutenberg University
Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.
Kyushu University
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
Shandong University
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.
Boehringer Ingelheim (Canada)
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
University of Southern California
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Eli Lilly
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
Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies.
Johannes Gutenberg University
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
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Novartis Institute of Biomedical Research
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.
Ligand Pharmaceuticals
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.
Abbott
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.
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.
Senju Pharmaceutical
N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.
University of Bonn
Synthesis and matched molecular pair analysis of covalent reversible inhibitors of the cysteine protease CPB.
S£O Carlos Institute of Chemistry-University of S£O Paulo (Iqsc-Usp)
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
Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
Ewha Womans University
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
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Pfizer
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.
Abbott
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
University of California
Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.
University of S£O Paulo
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Novartis Pharmaceuticals
Cytotoxicity of 4-substituted quinoline derivatives: Anticancer and antileishmanial potential.
Universidade De Mogi Das Cruzes (Umc)
Potent reversible inhibitors of the protein tyrosine phosphatase CD45.
Astrazeneca Pharmaceuticals
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.
Merck Frosst Centre For Therapeutic Research
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.
The University of Tennessee Health Science Center
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Roche Pharma Research and Early Development
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.
Knoll
Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.
Queen'S University Belfast
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.
Brown University
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.
National Institute of Biological Sciences (Nibs)
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.
Jilin University
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.
Boehringer Ingelheim (Canada)
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.
Boehringer Ingelheim (Canada)
Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe.
Ku Leuven
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.
Texas A&M University
Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor.
University of Nebraska Medical Center
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
Cathepsin B: Active site mapping with peptidic substrates and inhibitors.
University of Bonn
Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?
University of S£O Paulo
Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments.
University of Houston
Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.
Georgia Institute of Technology
Development of a potent and selective cell penetrant Legumain inhibitor.
Queen'S University Belfast
Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.
Sichuan University
Peptide alpha-keto ester, alpha-keto amide, and alpha-keto acid inhibitors of calpains and other cysteine proteases.
Georgia Institute of Technology
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
University of California
Development of cell-active non-peptidyl inhibitors of cysteine cathepsins.
The City University of New York
Chalcones, inhibitors for topoisomerase I and cathepsin B and L, as potential anti-cancer agents.
Cha University
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?
National Institute of Biology
Small-molecule inhibitors of cathepsin L incorporating functionalized ring-fused molecular frameworks.
Baylor University
Shishicrellastatins, inhibitors of cathepsin B, from the marine sponge Crella (Yvesia) spinulata.
The University of Tokyo
New aziridine-based inhibitors of cathepsin L-like cysteine proteases with selectivity for the Leishmania cysteine protease LmCPB2.8.
Johannes Gutenberg-Universit£T Mainz
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.
Orleans University
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates.
Universitat Jaume I
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Irbm Science Park
Cathepsin B inhibitors: Further exploration of the nitroxoline core.
University of Ljubljana
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.
Eth Zurich
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
Idiopathic Pulmonary Fibrosis: Current Status, Recent Progress, and Emerging Targets.
Taipei Medical University
Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases
Rockefeller University
Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
Sk Biopharmaceuticals
Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
Bristol-Myers Squibb
Use of small molecule inhibitors targeting EYA tyrosine phosphatase
Cincinnati Childrens Hospital Medical Center
Piperidine substituted tricyclic pyrazolo[1,5-a]pyrimidine derivatives with inhibitory activity on the replication of the respiratory syncytial virus (RSV)
Janssen Ireland
Bicyclic heteroaryl derivatives as CFTR potentiators
Cystic Fibrosis Foundation Therapeutics
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases
Galderma Research & Development
Pharmacologic characterization of CI-996, a new angiotensin receptor antagonist.
Parke-Davis Pharmaceutical Research
Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells.
Mayo Clinic
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.
Cyclacel
Thermodynamic and Nuclear Magnetic Resonance Study of the Reactions of α- and β-Cyclodextrin with Acids, Aliphatic Amines, and Cyclic Alcohols
Nist
Design, synthesis, and evaluation of novel organophosphorus inhibitors of bacterial ureases.
Wroclaw University of Technology
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition.
University of Dundee
Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.
Pfizer
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.
Glaxosmithkline
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Merck Research Laboratories
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.
Astrazeneca
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.
Institut Curie
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.
Korea Research Institute of Bioscience and Biotechnology