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135 articles for thisTarget

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

Article Title
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.EBI
Carna Biosciences
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.EBI
Comenius University In Bratislava
Novel GSK-3 inhibitors with improved cellular activity.EBI
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors.EBI
Paris-Sud University
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.EBI
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).EBI
Icahn School of Medicine At Mount Sinai
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.EBI
Central University
Evaluation of Improved Glycogen Synthase Kinase-3a Inhibitors in Models of Acute Myeloid Leukemia.EBI
Technische Universit£T Darmstadt
Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.EBI
University of Cambridge
Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.EBI
Eli Lilly
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.EBI
The Institute of Cancer Research
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI
Vertex Pharmaceuticals
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.EBI
Technische Universit£T Darmstadt
The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.EBI
University of Dundee
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.EBI
Universitat De Barcelona
3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3.EBI
Technische Universit£T Braunschweig
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI
Abbott Laboratories
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.EBI
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.EBI
Identification of pyrimidine derivatives as hSMG-1 inhibitors.EBI
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI
Abbott Laboratories
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.EBI
Technische Universit£T Darmstadt
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI
Abbott Laboratories
Pharmacological inhibitors of glycogen synthase kinase 3.EBI
The Rockefeller University
Discovery of potent and bioavailable GSK-3beta inhibitors.EBI
Roche Palo Alto
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Kinetic studies and bioactivity of potential manzamine prodrugs.EBI
The University of Mississippi
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).EBI
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI
Abbott Laboratories
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI
Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.EBI
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.EBI
Technische Universit£T Darmstadt
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.EBI
National University of Ireland
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.EBI
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.EBI
Abbott Laboratories
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI
Wyeth Research
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI
Abbott Laboratories
Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.EBI
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.EBI
Roche Research Center
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.EBI
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.EBI
Massachusetts General Hospital
Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.EBI
Zunyi Medical University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.EBI
Hefei University of Technology
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.EBI
Johnson & Johnson Pharmaceutical Research and Development
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.EBI
Hefei University of Technology
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.EBI
University of Dundee
Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review.EBI
University of Louisiana At Lafayette
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.EBI
Indian Institute of Technology (B.H.U.)
A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing.EBI
China Pharmaceutical University
Discovery of (EBI
Bristol-Myers Squibb
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer.EBI
Bayer Pharma
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.EBI
University of Campinas (Unicamp)
Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers.EBI
Carna Biosciences
Discovery of EBI
China Pharmaceutical University
A novel GSK-3 inhibitor binds to GSK-3? via a reversible, time and Cys-199-dependent mechanism.EBI
Ohio University
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.EBI
University Paris-Saclay
Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.EBI
University of South Australia
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.EBI
Beijing Normal University
An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.EBI
University of Oxford
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.EBI
China Pharmaceutical University
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.EBI
China Pharmaceutical University
Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series.EBI
University of North Carolina
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.EBI
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and EBI
Angelini Pharma
Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures.EBI
The First Affiliated Hospital of Zhengzhou University
Kinase-Inhibitory Nucleoside Derivatives from the Pacific Bryozoan EBI
Victoria University of Wellington
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.EBI
Pyridinylimidazoles as dual glycogen synthase kinase 3?/p38? mitogen-activated protein kinase inhibitors.EBI
Eberhard Karls Universit£T T£Bingen
Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.EBI
Jamia Hamdard
1-Aryl-3-(4-methoxybenzyl)ureas as potentially irreversible glycogen synthase kinase 3 inhibitors: Synthesis and biological evaluation.EBI
Stellenbosch University
Discovery of 4EBI
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.EBI
Vertex Pharmaceuticals (Europe)
Discovery of novel glycogen synthase kinase-3? inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.EBI
Peking University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI
University of Florida
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI
Abbvie Bioresearch Center
Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme.EBI
University of Pisa
Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors.EBI
Jeil Pharmaceutical
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.EBI
Vertex Pharmaceuticals
The development of potent and selective bisarylmaleimide GSK3 inhibitors.EBI
Lilly Research Laboratories
3D QSAR studies on GSK-3 inhibition by aloisines.EBI
Zhejiang University
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.EBI
Seoul National University
Glycogen synthase kinase-3 and its inhibitors: Potential target for various therapeutic conditions.EBI
National Institute of Pharmaceutical Education and Research (NIPER)
Natural and synthetic bioactive inhibitors of glycogen synthase kinase.EBI
Jamia Hamdard (Hamdard University)
Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.EBI
Novartis Institutes For Biomedical Research
Designing modulators of dimethylarginine dimethylaminohydrolase (DDAH): a focus on selectivity over arginase.BDB
Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.BDB
Shandong University
Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.BDB
University of Alexandria
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.BDB
Eli Lilly
Development of new and selective Trypanosoma cruzi trans-sialidase inhibitors from sulfonamide chalcones and their derivatives.BDB
University of British Columbia
Synthesis and molecular modelling of novel substituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase-A inhibitors.BDB
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.BDB
Smithkline Beecham Pharmaceuticals
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.BDB
Wyeth Research
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.BDB
Abbott Laboratories
Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.BDB
Sapienza University of Rome
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships.BDB
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 1. Structure-Activity Relationships and Optimization of Heterocyclic Substituents.BDB
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.BDB
University of Arizona Tucson
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.BDB
Novartis Pharmaceuticals
Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.BDB
Hebrew University of Jerusalem