108 articles for thisTarget
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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
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.
Sri International
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.
Comenius University In Bratislava
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
Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.
University of Clermont Auvergne
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
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
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Technische Universit£T Braunschweig
Synthesis and molecular modelling studies of 8-arylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amines as multitarget Ser/Thr kinases inhibitors.
Cobra
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
Synthesis, biological evaluation and molecular modelling studies of 4-anilinoquinazoline derivatives as protein kinase inhibitors.
Rajiv Gandhi Proudyogiki Vishwavidyalaya
Synthesis of novel 7-substituted pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues and evaluation of their inhibitory activity against Ser/Thr kinases.
Cobra
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.
University of Rennes 1
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
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
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.
University of Rouen Normandy
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.
TBA
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.
Cellzome
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Cnrs
Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors.
University of Rouen Normandy
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of analogs of the marine alkaloids granulatimide and isogranulatimide.
Paul Sabatier University
Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases.
Institut De Chimie Des Substances Naturelles (Icsn)
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.
Boehringer Ingelheim Pharmaceuticals
Synthesis, protein kinase inhibitory potencies, and in vitro antiproliferative activities of meridianin derivatives.
Clermont Universite£
Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Universite£? De Rennes 1
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Trinity 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
6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3ß inhibitors.
Pfizer
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
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.
Paris-Sud University
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
National Human Genome Research Institute
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?
Pfizer
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI).
West China Hospital of Sichuan University
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.
Insilico Medicine Shanghai
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Perha Pharmaceuticals
Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
National Cancer Institute
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Perha Pharmaceuticals
Discovery of novel 5-methoxybenzothiophene hydrazides as metabolically stable Clk1 inhibitors with high potency and unprecedented Clk1 isoenzyme selectivity.
German University In Cairo
Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases.
University of Rouen Normandy
MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core.
Goethe University Frankfurt
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
β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
Fused-azepinones: Emerging scaffolds of medicinal importance.
National Institute of Pharmaceutical Education and Research (NIPER)
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
University of Clermont Auvergne
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Bristol-Myers Squibb
DYRK1A inhibitors for disease therapy: Current status and perspectives.
West China Hospital
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
Recent advances in the development of active hybrid molecules in the treatment of cardiovascular diseases.
Western University of Health Sciences
Development of novel conformationally restricted selective Clk1/4 inhibitors through creating an intramolecular hydrogen bond involving an imide linker.
German University In Cairo
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
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
Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.
Vernalis (R&D)
Discovery of thiazolidin-4-one analogue as selective GSK-3β inhibitor through structure based virtual screening.
Central University of Rajasthan
Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers.
Carna Biosciences
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors.
Sichuan University
In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition.
University of Nantes
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.
University of Sussex
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.
Paris-Saclay University
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.
Masaryk University
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
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.
University of Michigan
Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.
Chemveda Life Sciences India
New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis.
University of Clermont Auvergne
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and
Angelini Pharma
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.
University of Naples Federico Ii
Kinase inhibitions in pyrido[4,3-h] and [3,4-g]quinazolines: Synthesis, SAR and molecular modeling studies.
University of Clermont Auvergne
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
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88
Astrazeneca
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
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 β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.
University of Poitiers
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.
Seoul National University
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Astrazeneca
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.
University of Tours
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.
University of Nantes
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
University of Paris
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
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88
Astrazeneca
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε 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
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.
Takeda Chemical Industries