164 articles for thisTarget
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Article Title
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Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.
Sichuan University and Collaborative Innovation Center For Biotherapy
Discovery of novel furanone derivatives as potent Cdc7 kinase inhibitors.
Carna Biosciences
Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma.
Qimr Berghofer Medical Research Institute
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.
East China Normal University
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.
Comenius University In Bratislava
Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.
Astrazeneca
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.
Cnrs
Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors.
Paris-Sud University
Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.
Astrazeneca
Novel optimization of valmerins (tetrahydropyrido[1,2-a]isoindolones) as potent dual CDK5/GSK3 inhibitors.
Universit£
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.
Saarland University
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).
Icahn School of Medicine At Mount Sinai
Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.
Cnrs Umr 7311
Meridianin derivatives as potent Dyrk1A inhibitors and neuroprotective agents.
India Academy of Scientific & Innovative Research (Acsir)
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Technische Universit£T Braunschweig
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Astrazeneca
Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors.
Universit£
Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4.
Saarland University
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.
Institut De Chimie Des Substances Naturelles
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.
Technische Universit£T Braunschweig
Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity.
Upr 2301, Cnrs
Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Hoffmann-La Roche
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.
Universit£
Synthesis, resolution, and biological evaluation of atropisomeric (aR)- and (aS)-16-methyllamellarins N: unique effects of the axial chirality on the selectivity of protein kinases inhibition.
Nagasaki University
Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
University of Kansas Specialized Chemistry Center
Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease.
Dart Neuroscience
Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases.
Universit£
Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling.
University of Paris
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.
TBA
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
Universit£
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Cnrs
Novel trisubstituted harmine derivatives with original in vitro anticancer activity.
University of Namur (Fundp)
A one-pot synthesis and biological activity of ageladine A and analogues.
Macquarie University
Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.
Harvard Medical School
Butyrolactone I derivatives from Aspergillus terreus carrying an unusual sulfate moiety.
Leibniz-Institute For Natural Product Research and Infection Biology
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Discovery of potent small molecule inhibitors of DYRK1A by structure-based virtual screening and bioassay.
The Second Military Medical University
A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.
Imperial College
Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).
National Human Genome Research Institute
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
8-Hydroxynaphthalene-1,4-dione derivative as novel compound for glioma treatment.
University of Padova
Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.
Martin-Luther-University Halle-Wittenberg
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
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.
Abbott Laboratories
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
National Human Genome Research Institute
Identification of death-associated protein kinases inhibitors using structure-based virtual screening.
Pharmadesign
Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors.
Laboratorio De Radicales Libres Y QuÍMica Computacional (Iqog, Csic)
QSAR analysis of pyrazolidine-3,5-diones derivatives as Dyrk1A inhibitors.
Inje University
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening.
Università
5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.
Danylo Halytsky Lviv National Medical University
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.
University of North Carolina At Chapel Hill
DYRK1A kinase inhibition with emphasis on neurodegeneration: A comprehensive evolution story-cum-perspective.
Jamia Hamdard
Silmitasertib (CX-4945), a Clinically Used CK2-Kinase Inhibitor with Additional Effects on GSK3? and DYRK1A Kinases: A Structural Perspective.
Jagiellonian University
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
Perha Pharmaceuticals
Development of Cdc2-like Kinase 2 Inhibitors: Achievements and Future Directions.
China Pharmaceutical University
DYRK1A Inhibitors as Potential Therapeutics for ?-Cell Regeneration for Diabetes.
Icahn School of Medicine At Mount Sinai
?-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
A review: Biologically active 3,4-heterocycle-fused coumarins.
Tehran University of Medical Sciences
Fused-azepinones: Emerging scaffolds of medicinal importance.
National Institute of Pharmaceutical Education and Research (NIPER)
Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.
Università
ARN25068, a versatile starting point towards triple GSK-3?/FYN/DYRK1A inhibitors to tackle tau-related neurological disorders.
University of Bologna
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling.
University College London
Discovery of novel benzothiophene derivatives as potent and narrow spectrum inhibitors of DYRK1A and DYRK1B.
Ach£
Design, synthesis, and biological evaluation of polyphenol derivatives as DYRK1A inhibitors. The discovery of a potentially promising treatment for Multiple Sclerosis.
Avanti Biosciences
Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/?-synuclein aggregation inhibitors with neuroprotective effects.
German University In Cairo
DYRK1A inhibitors for disease therapy: Current status and perspectives.
West China Hospital
Structure-activity relationship for the folding intermediate-selective inhibition of DYRK1A.
Shinshu University
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
Glaxosmithkline
Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors.
Manros Therapeutics & Perha Pharmaceuticals
Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review.
University of Louisiana At Lafayette
Development of novel conformationally restricted selective Clk1/4 inhibitors through creating an intramolecular hydrogen bond involving an imide linker.
German University In Cairo
Screening of a Halogen-Enriched Fragment Library Leads to Unconventional Binding Modes.
Eberhard Karls Universit£T T£Bingen
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.
China Pharmaceutical University
Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.
Università
Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
Servier Research Institute of Medicinal Chemistry
Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.
Vernalis (R&D)
Discovery of thiazolidin-4-one analogue as selective GSK-3? inhibitor through structure based virtual screening.
Central University of Rajasthan
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3?/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.
Shenyang Pharmaceutical University
Synthesis of novel 1H-Pyrazolo[3,4-b]pyridine derivatives as DYRK 1A/1B inhibitors.
Yonsei University
Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors.
Sichuan University
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.
University of Sussex
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.
Masaryk University
Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome.
Usona Institute
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.
Goethe-University Frankfurt
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
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.
University of Oxford
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
China Pharmaceutical University
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
China Pharmaceutical University
Discovery of DS42450411 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4-aminopyrimidine derivatives.
Daiichi Sankyo
Probing the ATP-Binding Pocket of Protein Kinase DYRK1A with Benzothiazole Fragment Molecules.
Uit The Arctic University of Norway
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and
Angelini Pharma
Generation of highly potent DYRK1A-dependent inducers of human ?-Cell replication via Multi-Dimensional compound optimization.
Stanford University
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Genomics Institute of The Novartis Research Foundation (Gnf)
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site.
Saarland University
2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.
Universit£
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.
University of Padova
Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human ?-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.
Icahn School of Medicine At Mount Sinai
Kinase Chemodiversity from the Arctic: The Breitfussins.
Uit - The Arctic University of Norway
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
University of Florida
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abbvie Bioresearch Center
Development of novel amide-derivatized 2,4-bispyridyl thiophenes as highly potent and selective Dyrk1A inhibitors. Part II: Identification of the cyclopropylamide moiety as a key modification.
German University In Cairo
A ?-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.
Universit£
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.
Seoul National University
Development of novel 2,4-bispyridyl thiophene-based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives.
German University In Cairo
Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic ?-cell proliferation activity.
Icahn School of Medicine At Mount Sinai
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.
Uit The Arctic University of Norway
Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human ?-Cell Proliferation.
TBA
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
University of Paris
Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.
Rigel Pharmaceuticals
The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen.
Celgene
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1?/? inhibitors: Synthesis, biological evaluation and molecular modeling studies.
Rajiv Gandhi Proudyogiki Vishwavidyalaya
Development of Selective Clk1 and -4 Inhibitors for Cellular Depletion of Cancer-Relevant Proteins.
German University In Cairo
Benzobisthiazoles Represent a Novel Scaffold for Kinase Inhibitors of CLK Family Members.
University College London