99 articles for thisTarget
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Article Title
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Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Enriching screening libraries with bioactive fragment space.
Beijing University of Technology
Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.
Astrazeneca
Computational Tools To Model Halogen Bonds in Medicinal Chemistry.
Colorado State University
Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.
Kyoto University
Synthesis of novel polybrominated benzimidazole derivatives-potential CK2 inhibitors with anticancer and proapoptotic activity.
Warsaw University of Technology
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
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.
Christian-Albrechts-University of Kiel
Synthesis of novel chiral TBBt derivatives with hydroxyl moiety. Studies on inhibition of human protein kinase CK2a and cytotoxicity properties.
Warsaw University of Technology
Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
Siedlce University of Natural Sciences and Humanities
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
Astrazeneca
Trimeric hemibastadin congener from the marine sponge Ianthella basta.
Heinrich-Heine University
Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds.
Kyoto University
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
Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.
Cylene Pharmaceuticals
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
TBA
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.
Institute For Biochemistry
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.
Millennium Pharmaceuticals
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Osi Pharmaceuticals
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
CK2a and CK2a' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.
The John Paul Ii Catholic University of Lublin
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Cylene Pharmaceuticals
Identification of potent ITK inhibitors through focused compound library design including structural information.
Nycomed
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.
Osaka Prefecture University
Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2.
Institute of Biochemistry and Biophysics
Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Eberhard-Karls University
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors.
Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water.
Kindai University
Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.
Sichuan University
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
Polaris Pharmaceuticals
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Biocon-Bristol Myers Squibb Research and Development Center
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.
University of North Carolina at Chapel Hill
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-
Biocon-Bristol Myers Squibb Research and Development Center
Silmitasertib (CX-4945), a Clinically Used CK2-Kinase Inhibitor with Additional Effects on GSK3β and DYRK1A Kinases: A Structural Perspective.
Jagiellonian University
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-
Goethe University Frankfurt
Molecular Plasticity of Crystalline CK2α' Leads to KN2, a Bivalent Inhibitor of Protein Kinase CK2 with Extraordinary Selectivity.
Universit£T Zu K£Ln
A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.
University of Cambridge
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
University of North Carolina at Chapel Hill
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
Michigan State University
A novel class of selective CK2 inhibitors targeting its open hinge conformation.
University of Trento
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.
Goethe University Frankfurt
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.
Mansoura University
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity
University of Nottingham
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.
Japan Tobacco
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.
University of Lyon
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
Small molecule modulators targeting protein kinase CK1 and CK2.
China Pharmaceutical University
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 Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Dana-Farber Cancer Institute
Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.
Heinrich-Heine-Universitat
Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.
Heinrich-Heine-Universit£T
A new family of densely functionalized fused-benzoquinones as potent human protein kinase CK2 inhibitors.
Instituto Universitario De Bio-Org£Nica Antonio Gonz£Lez (Cibican)
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
Identification by Inverse Virtual Screening of magnolol-based scaffold as new tankyrase-2 inhibitors.
University of Salerno
Novel non-ATP competitive small molecules targeting the CK2 α/β interface.
University of Cambridge
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Astrazeneca
Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.
University of Tartu
Oligo-aspartic acid conjugates with benzo[c][2,6]naphthyridine-8-carboxylic acid scaffold as picomolar inhibitors of CK2.
University of Tartu
A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066.
University of Cambridge
Benzo[c][2,6]naphthyridine derivatives, compositions and therapeutic uses thereof
Cambridge Enterprise
INDOLE DERIVATIVES AND USES THEREOF FOR TREATING A CANCER
Universite Claude Bernard Lyon 1
Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives.
Warsaw University of Technology
Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
Senhwa Biosciences
Structural basis for low-affinity binding of non-R2 carboxylate-substituted tricyclic quinoline analogs to CK2a: comparative molecular dynamics simulation studies.
Beijing University of Technology
De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.
University of Dundee
Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.
Venetian Institute of Molecular Medicine
A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis.
Nagoya University School of Medicine
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells.
Nagoya University School of Medicine
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).
University of Padova