284 articles for thisTarget
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Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
Hoffmann-La Roche
Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Hoffmann-La Roche
Discovery of novel non-carboxylic acid 5-amino-4-cyanopyrazole derivatives as potent and highly selective LPA1R antagonists.
Hoffmann-La Roche
Discovery of camphor-derived pyrazolones as 11ß-hydroxysteroid dehydrogenase type 1 inhibitors.
Hoffmann-La Roche
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.
Hoffmann-La Roche
Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Hoffmann-La Roche
Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.
Hoffmann-La Roche
Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.
Hoffmann-La Roche
Discovery of a novel series of potent non-nucleoside inhibitors of hepatitis C virus NS5B.
Hoffmann-La Roche
Design and synthesis of 2-N-substituted indazolone derivatives as non-carboxylic acid glycogen synthase activators.
Hoffmann-La Roche
Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.
Hoffmann-La Roche
Identification of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives and their orally active prodrug esters as dual-acting alpha4-beta1 and alpha4-beta7 receptor antagonists.
Hoffmann-La Roche
Identification of N-acyl 4-(3-pyridonyl)phenylalanine derivatives and their orally active prodrug esters as dual actinga4ß1 anda4ß7 receptor antagonists.
Hoffmann-La Roche
Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.
Hoffmann-La Roche
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
Hoffmann-La Roche
N-acyl-L-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation.
Hoffmann-La Roche
Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists.
Hoffmann-La Roche
N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
Hoffmann-La Roche
Rational design of highly selective spleen tyrosine kinase inhibitors.
Hoffmann-La Roche
Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
Hoffmann-La Roche
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.
Hoffmann-La Roche
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
Hoffmann-La Roche
Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.
Hoffmann-La Roche
RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.
Hoffmann-La Roche
Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors.
Hoffmann-La Roche
Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.
Hoffmann-La Roche
Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.
Hoffmann-La Roche
Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs.
Hoffmann-La Roche
A potent seven-membered cyclic BTK (Bruton's tyrosine Kinase) chiral inhibitor conceived by structure-based drug design to lock its bioactive conformation.
Hoffmann-La Roche
Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.
Hoffmann-La Roche
Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs.
Hoffmann-La Roche
Pyrido[2,1-b]quinazolinecarboxamide derivatives as platelet activating factor antagonists.
Hoffmann-La Roche
Propenyl carboxamide derivatives as antagonists of platelet activating factor.
Hoffmann-La Roche
STING MODULATOR COMPOUNDS WITH SULFAMATE LINKAGES, AND METHODS OF MAKING AND USING
Takeda Pharmaceutical
3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl) propanenitrile as a JAK kinase inhibitor
Theravance Biopharma R&D IP
COMPOUNDS FOR INHIBITING INOSITOL HEXAKISPHOSPHATE KINASE (IP6K) AND METHODS OF USE THEREOF
Lieber Institute
Pyrazolo[3,4-d]pyrrolo[1,2-b]pyridazinyl compounds useful as IRAK4 inhibitors
Bristol-Myers Squibb
INHIBITORS OF SERINE/THREONINE PROTEIN KINASE STK3 OR STK4 AND USES THEREOF
Sanford Burnham Prebys Medical Discovery Institute
CYCLIC SULFONAMIDE RIBONUCLEOTIDE REDUCTASE (RNR) INHIBITORS AND USES THEREOF
Boundless Bio
Azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
Hoffmann-La Roche
Polycyclic carbamoylpyridone derivatives, pharmaceutical compositions and use thereof
Jiaxing Andicon Biotech Co.
PROCESS FOR THE MANUFACTURE OF (2S,3S,4S,5R,6S)-3,4,5-TRIHYDROXY-6-(((4AR,10AR)-7-HYDROXY-1-PROPYL-1,2,3,4,4A,5,10,10A-OCTAHYDROBENZO[G]QUINOLIN-6-YL)OXY)TETRAHYDRO-2H-PYRAN-2-CARBOXYLIC ACID
H. Lundbeck
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF IN MEDICINES
Jiangsu Hengrui Pharmaceuticals
RECEPTOR-INTERACTING PROTEIN INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF
Chengdu Biobel Biotechnology Co.
ANTIBIOTICS COMPRISING LPXH-TARGETING COMPOUNDS AND METHODS OF MAKING AND USING THE SAME
Duke University
PRIDOPIDINE AND ANALOGS THEREOF FOR THE TREATMENT OF NEURODEGENERATIVE EYE DISEASE
Prilenia Neurotherapeutics
PREPARATION OF FUSED AZOLE DERIVATIVES AS NOVEL DIACYLGLYCERIDE 0-ACYLTRANSFERASE 2 INHIBITORS
Merck Sharp & Dohme
COMPOUND HAVING BIOLOGICAL ACTIVITY SUCH AS ANTIVIRAL ACTIVITY
National Center For Global Health And Medicine
NITROGEN-CONTAINING POLYCYCLIC FUSED RING COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF
Applied Pharmaceutical Science
PYRIMIDINONE-CONTAINING 17-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 13 INHIBITORS
Enanta Pharmaceuticals
5-SUBSTITUTED INDOLE 3-AMIDE DERIVATIVES, PREPARATION METHOD AND USE THEREOF
Origiant Pharmaceutical
NOVEL PHARMACOLOGICAL CHAPERONE COMPOUNDS OF HUMAN ACID ALPHA-GLUCOSIDASE AND THE THERAPEUTIC USE THEREOF
UniversitÉ
Substituted pyrazolopyrazines, imidazopyrazines and [1,2,4]triazolopyrazines as allosteric SHP2 inhibitors
Revolution Medicines
Azole derivatives as apelin receptor agonist
Sanford Burnham Prebys Medical Discovery Institute
FAP-targeted radiopharmaceuticals and imaging agents, and uses related thereto
Tufts College
Substituted benzoxazole and benzofuran compounds as PDE7 inhibitors
Dart Neuroscience
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma
RIP1 inhibitory compounds and methods for making and using the same
Rigel Pharmaceuticals
Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals
Bayer Animal Health
Zwitterionic propargyl-linked antifolates useful for treating bacterial infections
University of Connecticut
Compositions and methods for inhibiting brain trauma-induced neurodegeneration and related conditions
Aristea Translational Medicine
Pyridine derivative inhibiting RAF kinase and vascular endothelial growth factor receptor, method for preparing same, pharmaceutical composition containing same, and use thereof
Incheon University Industry Academic Cooperation Foundation
Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
Incyte
N-((het) arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors
Kalvista Pharmaceuticals
1,1 ′-sulfanediyl-di-beta-D-galactopyranosides as inhibitors of galectins
Galecto Biotech
Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-A]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
Ogeda
Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals
Curcumin analogues as zinc chelators and their uses
The Research Foundation of State University of New York
6-(5-membered heteroaryl)isoquinolin-3-yl carboxamides and preparation and use thereof
Samumed
Tetrahydropyrimidodiazepine and dihydropyridodiazepine compounds for treating pain and pain related conditions
Esteve Pharmaceuticals
Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines and substituted imidazo[1,2-b]pyridazines as PI3K-gamma inhibitors
Incyte
Cyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide
Boehringer Ingelheim International
Tetrahydroquinoline substituted hydroxamic acids as selective histone deacetylase 6 inhibitors
University of Illinois
Imidazo[4,5-C]pyridine and pyrrolo[2,3-C]pyridine derivatives as SSAO inhibitors
Proximagen
Use of agonists of formyl peptide receptor 2 for treating dermatological diseases
Allergan
Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
Boehringer Ingelheim International
Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
Lycera
Modulation of N-acylethanolamine-hydrolysing acid amidase (NAAA) for disease treatment
Fondazione Istituto Italiano Di Tecnologia
Pyrazolopyrimidone or Pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof
Shanghai Hengrui Pharmaceutical
Plasminogen activator inhibitor-1 inhibitors and methods of use thereof
University of Michigan
Galactokinase inhibitors for the treatment and prevention of associated diseases and disorders
University of Utah
Substituted pyrrolidines as factor xia inhibitors for the treatment thromboembolic diseases
Ono Pharmaceutical
Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold.
Nanchang University School of Pharmaceutical Science
Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cell migration.
University of Colorado School of Medicine
Design, synthesis and biological activity of 3-oxoamino-benzenesulfonamides as selective and reversible LSD1 inhibitors.
China Pharmaceutical University
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of novel flavanone derivatives as potential antipsychotic agents.
Key Laboratory For Neurodegenerative Diseases of Ministry of Education
Molecular characterization of zebrafish Oatp1d1 (Slco1d1), a novel organic anion-transporting polypeptide.
Rudjer Boskovic Institute
Discovery and Characterization of Allosteric WNK Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality
Genentech
Inhibition of the Flavin-Dependent Monooxygenase Siderophore A (SidA) Blocks Siderophore Biosynthesis and Aspergillus fumigatus Growth.
Virginia Tech
Aniline derivatives, their preparation and their therapeutic application
Fovea Pharmaceuticals
Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives
Reviva Pharmaceuticals
Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently.
Korea Institute of Science and Technology
3-[4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane—or heptane-nitrile as JAK inhibitors
Incyte
Structural insights into HDAC6 tubulin deacetylation and its selective inhibition.
Friedrich Miescher Institute For Biomedical Research
Structural analysis of human KDM5B guides histone demethylase inhibitor development.
University of Oxford
A simple and efficient synthesis of novel inhibitors of alpha-glucosidase based on benzimidazole skeleton and molecular docking studies.
Recep Tayyip Erdogan University
Synthesis, ß-glucuronidase inhibition and molecular docking studies of hybrid bisindole-thiosemicarbazides analogs.
Universiti Teknologi Mara
2-substituted-3-phenylpropionic acid derivatives and their use in the treatment of inflammatory bowel disease
Albireo
A Novel Inhibitor of the Obesity-Related Protein FTO.
Basic Medical College of Zhengzhou University
Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel.
Novartis Institutes of Biomedical Research Institute
Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
Albany Molecular Research
Design, synthesis, and biological evaluation of scutellarein carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
Boehringer Ingelheim International
Fluoro-substituted 2-aryl-3,5-dicyano-4-indazolyl-6-methyl-1,4-dihydropyridines and uses thereof
Bayer Intellectual Property
Methods of modifying amyloid β oligomers using non-peptidic compounds
Acumen Pharmaceuticals
Discovery of novel 17-phenylethylaminegeldanamycin derivatives as potent Hsp90 inhibitors.
Shandong University
Development of fluorinated methoxylated chalcones as selective monoamine oxidase-B inhibitors: Synthesis, biochemistry and molecular docking studies.
Grace College of Pharmacy
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes.
Comsats Institute of Information Technology
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Abbvie
Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
Bristol-Myers Squibb
2,3-dihydro-1H-indene-2-yl urea derivative and pharmaceutical application of same
Toray Industries
Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
Merck Sharp & Dohme
Quinazoline derivatives as a multiplex inhibitor and method for the preparation thereof
Hanmi Pharm.
6-cyclylmethyl-and 6-alkylmethyl-substituted pyrazolepyrimidines
Boehringer Ingelheim International
Diamide compounds having muscarinic receptor antagonist and β2 adrenergic receptor agonist activity
Theravance Respiratory
Sulfone-substituted anilinopyrimidine derivatives as CDK inhibitors, the production thereof, and use as a medicine
Bayer Intellectual Property
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors
Array Biopharma
Bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives and uses thereof
Bayer Intellectual Property
Synthesis and xanthine oxidase inhibitory activity of 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives.
Central University of Punjab
Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
Merck Sharp & Dohme
Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
Universidad Del PaíS Vasco
The adenosine A(2A) antagonistic properties of selected C8-substituted xanthines.
North-West University, Private Bag X6001, Potchefstroom 2520, South Africa
Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof
Japan Tobacco
Identification of type II inhibitors targeting BRAF using privileged pharmacophores.
Shanghai Institute of Pharmaceutical Industry
Synthesis, evaluation and molecular docking of prolyl-fluoropyrrolidine derivatives as dipeptidyl peptidase IV inhibitors.
Delhi Institute of Pharmaceutical Sciences and Research
Testing the substrate-envelope hypothesis with designed pairs of compounds.
Massachusetts Institute of Technology
Botryllamides and method of inhibiting PGP in a mammal afflicted with cancer
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.
University of Pittsburgh
Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases.
Spanish National Cancer Research Center (Cnio)
Reduced expression of CD45 protein-tyrosine phosphatase provides protection against anthrax pathogenesis.
United States Army Medical Research Institute of Infectious Diseases
Crystal structure of the Ca2+/calmodulin-dependent protein kinase kinase in complex with the inhibitor STO-609.
Riken Systems and Structural Biology Center
Inhibitory effects on mushroom tyrosinase by flavones from the stem barks of Morus lhou (S.) Koidz.
Gyeongsang National University
Pharmacological characterization of (E)-N-(4-fluorobut-2-enyl)-2beta-carbomethoxy-3beta-(4'-tolyl)nortropane (LBT-999) as a highly promising fluorinated ligand for the dopamine transporter.
University of Tours
Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2.
German Cancer Research Center
Pharmacological and genetic characterization of two selective serotonin transporter ligands: 2-[2-(dimethylaminomethylphenylthio)]-5-fluoromethylphenylamine (AFM) and 3-amino-4-[2-(dimethylaminomethyl-phenylthio)]benzonitrile (DASB).
National Institutes of Health
Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors.
University of Kentucky
The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin.
Merck Research Laboratories
In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.
Parke-Davis Pharmaceutical Research
Leflunomide's Bioactive Metabolite Has the Minimal Structural Requirements for the Efficient Inhibition of Human Dihydroorotate Dehydrogenase
Novartis Pharma
Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors.
University of Toronto
Affinity of various ligands for GABAA receptors containing alpha 4 beta 3 gamma 2, alpha 4 gamma 2, or alpha 1 beta 3 gamma 2 subunits.
University Clinic For Psychiatry
Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein.
Albany Medical College
Cloning, expression, and pharmacological characterization of a human alpha 2B-adrenergic receptor.
Neurogenetic
Biochemical and pharmacological properties of SR 46349B, a new potent and selective 5-hydroxytryptamine2 receptor antagonist.
Sanofi Recherche
Switching between allosteric and dimerization inhibition of HIV-1 protease.
Purdue University
Defining Cdk5 ligand chemical space with small molecule inhibitors of tau phosphorylation.
Harvard Medical School
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization.
Human Biomolecular Research Institute
Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.
Universita Di Siena
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.
Astrazeneca