108 articles for thisTarget
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Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
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
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.
Astellas Pharma
Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38a MAPK, CK1d and JAK2 kinase inhibitors.
Syncom
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.
Merck Research Laboratories
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
Difluoro-dioxolo-benzoimidazol-benzamides as potent inhibitors of CK1d ande with nanomolar inhibitory activity on cancer cell proliferation.
Ulm University Hospital
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.
Amgen
Protein kinase CK-1 inhibitors as new potential drugs for amyotrophic lateral sclerosis.
Csic
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Takeda Pharmaceutical
A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway.
University of Edinburgh Cancer Research Centre In The Institute of Genetics and Molecular Medicine
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.
The Institute of Cancer Research
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.
Merck Research Laboratories
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
Discovery of N6-phenyl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors using common-feature pharmacophore model based virtual screening and hit-to-lead optimization.
TBA
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Takeda Pharmaceutical
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
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
Amgen
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1¿) inhibitors.
Amgen
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.
Janssen Pharmaceutical Companies of Johnson & Johnson
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.
TBA
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.
Merck Research Laboratories
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
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.
Pfizer
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
Amgen
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.
Merck Research Laboratories
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.
The Institute of Cancer Research
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta.
Technische Universit£T Darmstadt
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
3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta.
Eberhard-Karls University
Identification of death-associated protein kinases inhibitors using structure-based virtual screening.
Pharmadesign
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Takeda Pharmaceutical
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening.
Università
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
Catecholamine Derivatives: Natural Occurrence, Structural Diversity, and Biological Activity.
Shandong University
Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ.
The Scripps Research Institute
Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions.
Janssen Research and Development
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Bristol-Myers Squibb Research & Development
Discovery of tricyclic dipyrrolopyridine derivatives as novel JAK inhibitors.
Astellas Pharma
High-Throughput Screening Platform in Postnatal Heart Cells and Chemical Probe Toolbox to Assess Cardiomyocyte Proliferation.
Christian-Albrechts University of Kiel
Rapid computational identification of the targets of protein kinase inhibitors.
University of Iowa
From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy.
The People'S Hospital of Xinjiang Uyghur Autonomous Region
Current progress and novel strategies that target CDK12 for drug discovery.
West China Hospital
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
Michigan State University
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.
Paris-Saclay University
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Sichuan University/Collaborative Innovation Center of Biotherapy
Developing novel classes of protein kinase CK1δ inhibitors by fusing [1,2,4]triazole with different bicyclic heteroaromatic systems.
University of Trieste
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.
Goethe-University Frankfurt
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.
Newcastle University
Scaffold Repurposing of in-House Chemical Library toward the Identification of New Casein Kinase 1 δ Inhibitors.
University of Padova
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ.
Korea Institute of Science and Technology
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.
Palack£
Discovering New Casein Kinase 1d Inhibitors with an Innovative Molecular Dynamics Enabled Virtual Screening Workflow.
Pfizer
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 A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abbvie Bioresearch Center
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Northwestern University
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Merck
Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε.
Ulm University Hospital
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
Scripps Florida
SALT OF 3,4-DIHYDROISOQUINOLINE COMPOUND AND USE THEREOF
CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang)
PREPARATION OF BIARYL RING-LINKED AROMATIC HETEROCYCLIC DERIVATIVE AS IMMUNOMODULATOR AND USE THEREOF
Shanghai Longwood Biopharmaceuticals
AROMATIC ETHYLENE COMPOUND AND PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
Guangzhou Maxinovel Pharmaceuticals
PYRROLO[2,1-F][1,2,4]TRIAZINES AND PREPARATION AND USES THEREOF
Biosplice Therapeutics
Heterocyclic compound as Syk inhibitor and/or Syk-HDAC dual inhibitor
Hangzhou Innogate Pharma
Methods of treatment using pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds
Array Biopharma
Substituted tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors
Phoenix Molecular Design
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.
Broad Institute
Activity based probes (ABPs) interacting with glycosidases
Academisch Medisch Centrum Bij Universiteit Van Amsterdam
Synthesis of tetramic and tetronic acids as beta-secretase inhibitors.
Darmstadt Technical University
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.
Universit&Aagrove
Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.
Merck Frosst Centre For Therapeutic Research
Factors controlling the complex architecture of native and modified cyclodextrins with dipeptide (Z-Glu-Tyr) studied by microcalorimetry and NMR spectroscopy: critical effects of peripheral bis-trimethylamination and cavity size.
Nagoya Institute of Technology