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142 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.EBI
East China Normal University
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.EBI
Sichuan University And Collaborative Innovation Center For Biotherapy
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI
Abbvie Bioresearch Center
Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.EBI
Newcastle University
Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.EBI
Comenius University In Bratislava
Non-kinase targets of protein kinase inhibitors.EBI
The University Of Sydney
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI
Merck
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.EBI
University Of Nebraska Medical Center
A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.EBI
India Academy Of Scientific & Innovative Research (Acsir)
Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).EBI
Astrazeneca
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.EBI
Genentech
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.EBI
Palack£
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.EBI
Chinese Academy Of Medical Sciences And Peking Union Medical College
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.EBI
University Of South Australia
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.EBI
The University Of Melbourne
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI
Astrazeneca
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.EBI
Technische Universit£T Braunschweig
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.EBI
Institut De Chimie Des Substances Naturelles
9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.EBI
Technische Universit£T Braunschweig
Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.EBI
Amgen
Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.EBI
Vichem Chemie
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.EBI
Amgen
Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.EBI
Universit£
Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.EBI
University Of Nottingham
6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.EBI
Universit£
Selectivity data: assessment, predictions, concordance, and implications.EBI
Eli Lilly
Lead identification of novel and selective TYK2 inhibitors.EBI
Genentech
A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.EBI
Palack£
Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.EBI
Boehringer Ingelheim (Canada)
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.EBI
H. Lee Moffitt Cancer Center And Research Institute
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.EBI
University Of Nottingham
Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.EBI
Palack£
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.EBI
University Of Oxford
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors.EBI
University Of St. Andrews
Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.EBI
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.EBI
Cellzome
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.EBI
Cnrs
Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents.EBI
University Of Nottingham
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthEBI
S Bio
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI
Abbott Laboratories
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI
Nerviano Medical Sciences Oncology
Discovery of potent and bioavailable GSK-3beta inhibitors.EBI
Roche Palo Alto
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI
Nerviano Medical Sciences
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.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
Synthesis and biological evaluation of benzo[d]imidazole derivatives as potential anti-cancer agents.EBI
University Of Nottingham
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI
Ansaris
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.EBI
The Institute Of Cancer Research
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI
University Of South Florida
The selective P-TEFb inhibitor CAN508 targets angiogenesis.EBI
Palack£
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.EBI
Imperial College
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.EBI
Trinity College
Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.EBI
Palacky£? University And Institute Of Experimental Botany Ascr
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI
Nerviano Medical Sciences
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
Cyclacel
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.EBI
Sunesis Pharmaceuticals
Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.EBI
Nerviano Medical Sciences
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.EBI
University Of Illinois At Chicago
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.EBI
Sunesis Pharmaceuticals
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.EBI
Banyu Tsukuba Research Institute
Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy.EBI
De Montfort University
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.EBI
Merck And
Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).EBI
Sanofi-Aventis Germany
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).EBI
Eli Lilly
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.EBI
Tianjin University Of Science And Technology
Discovery of CDK5 Inhibitors through Structure-Guided Approach.EBI
University Of South Australia
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.EBI
Palack£
Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor.EBI
Bayer
Discovery of 4EBI
TBA
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.EBI
Nankai University
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.EBI
Chengdu University
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.EBI
China Pharmaceutical University
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.EBI
China Pharmaceutical University
Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib.EBI
University Of Padova
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.EBI
University Of South Australia Cancer Research Institute
Kinase Chemodiversity from the Arctic: The Breitfussins.EBI
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.EBI
University Of Florida
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.EBI
Eppley Institute For Research In Cancer And Allied Diseases
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88EBI
Astrazeneca
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI
Takeda Pharmaceutical
3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights.EBI
Egyptian Russian University
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?EBI
Palack£
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.EBI
University Of South Australia
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.EBI
Novartis Institutes For Biomedical Research
Discovery of novel indirubin-3'-monoxime derivatives as potent inhibitors against CDK2 and CDK9.EBI
Chinese Academy Of Medical Sciences And Peking Union Medical College
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.EBI
Palack�
Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity.EBI
De Montfort University
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.EBI
Shanghai Pharmaceuticals Holding
A ?-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.EBI
Universit£
1,3,5-Triazines: A promising scaffold for anticancer drugs development.EBI
Universit£
Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.EBI
Central University Of Punjab
Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.EBI
Seoul National University
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.EBI
Astrazeneca
Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.EBI
Chinese Academy Of Sciences
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.EBI
University College Cork
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?EBI
University Of South Australia
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.EBI
Shanghai Haihe Pharmaceutical
Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro.EBI
China Pharmaceutical University
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.EBI
Chinese Academy Of Medical Sciences And Peking Union Medical College
Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.EBI
Semmelweis University
An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.EBI
University Of Kwazulu-Natal
Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.EBI
University Of Tours
Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.EBI
Takeda Pharmaceutical
Design, synthesis and biological evaluation of pyrimidine derivatives as novel CDK2 inhibitors that induce apoptosis and cell cycle arrest in breast cancer cells.EBI
Shihezi University
Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.EBI
Universit£
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.EBI
Nankai University
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.EBI
Csir-Indian Institute Of Integrative Medicine
Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.EBI
Sanofi Genzyme
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.EBI
Genentech
Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors.EBI
Korea Research Institute Of Chemical Technology
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.EBI
University Of Paris
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.EBI
Csir-Indian Institute Of Integrative Medicine
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.EBI
Takeda Pharmaceutical
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.EBI
Nankai University
N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1?/? inhibitors: Synthesis, biological evaluation and molecular modeling studies.EBI
Rajiv Gandhi Proudyogiki Vishwavidyalaya
[125I]Tyr10-cortistatin14 labels all five somatostatin receptors.BDB
Novartis Pharma
First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.BDB
Nerviano Medical Sciences
Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.BDB
Universite De Lyon
Synthetic and Crystallographic Studies of a New Inhibitor Series Targeting Bacillus anthracis Dihydrofolate Reductase.BDB
University Of Connecticut
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.BDB
Universita Di Pisa
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB
Palacky University
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.BDB
Cyclacel