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116 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28249207 78 Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.EBI East China Normal University
28692292 73 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
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
28005359 66 Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.EBI Newcastle University
27940419 31 Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands.EBI Comenius University in Bratislava
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck & Co.
27171036 164 Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.EBI University of Nebraska Medical Center
27363938 2 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)
27078757 121 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
26985305 34 Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.EBI Genentech Inc
26851505 65 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£ University and Institute of Experimental Botany AS CR
25914804 20 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
26408454 51 An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.EBI University of South Australia
26349627 133 Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.EBI The University of Melbourne
25262942 189 Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI AstraZeneca
25730262 195 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.EBI Technische Universit£t Braunschweig
24798019 30 Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.EBI Institut de Chimie des Substances Naturelles
24973661 10 9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.EBI Technische Universit£t Braunschweig
24793884 151 Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.EBI Amgen Inc
24742150 101 Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors.EBI Vichem Chemie Ltd.
24120542 90 The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.EBI Amgen Inc
23454515 66 Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.EBI Universit£ de Rennes1
24185375 76 Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.EBI University of Nottingham
23994326 9 6-Cyclohexylmethoxy-5-(cyano-NNO-azoxy)pyrimidine-4-amine: a new scaffold endowed with potent CDK2 inhibitory activity.EBI Universit£ degli Studi di Torino
23937569 22 Selectivity data: assessment, predictions, concordance, and implications.EBI Eli Lilly and Company
23867602 122 Lead identification of novel and selective TYK2 inhibitors.EBI Genentech
23829517 30 A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.EBI Palack£ University
23726345 41 Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.EBI Boehringer Ingelheim (Canada) Ltd
23600925 12 Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.EBI H. Lee Moffitt Cancer Center and Research Institute
23301767 154 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
22770608 35 Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.EBI Palack£ University
23252711 46 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
20146435 60 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
22982525 32 Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors.EBI TBA
22726925 216 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 Ltd
22998443 69 Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.EBI CNRS
23085105 30 Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents.EBI University of Nottingham
22339472 148 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 Pte. Ltd
22465635 95 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI Abbott Laboratories
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20138512 82 Discovery of potent and bioavailable GSK-3beta inhibitors.EBI Roche Palo Alto
20153204 109 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 srl
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18232649 60 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
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
22225635 5 Synthesis and biological evaluation of benzo[d]imidazole derivatives as potential anti-cancer agents.EBI University of Nottingham
22014550 337 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
21982796 108 Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.EBI The Institute of Cancer Research
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21907583 48 CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI University of South Florida
21777997 1 The selective P-TEFb inhibitor CAN508 targets angiogenesis.EBI Palack£ University & Institute of Experimental Botany ASCR
21080703 20 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
20621478 37 Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.EBI Trinity College
21417417 8 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
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences srl
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel Ltd
18842409 28 A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.EBI Sunesis Pharmaceuticals
19555113 45 Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.EBI Nerviano Medical Sciences
19338355 104 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
18926699 30 Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.EBI Sunesis Pharmaceuticals
16682184 25 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
28156111 214 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
27002243 42 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
25908517 14 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
25835357 22 Novel arylazopyrazole inhibitors of cyclin-dependent kinases.EBI Palack� University
25368960 17 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
30199702 24 A ?-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy.EBI Universit£ de Poitiers
29046238 17 1,3,5-Triazines: A promising scaffold for anticancer drugs development.EBI Universit£ degli Studi di Palermo
28911822 24 Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors.EBI Central University of Punjab
29985601 64 Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.EBI Seoul National University
29398441 111 Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.EBI AstraZeneca
30253346 46 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
30026041 139 Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.EBI University College Cork
29266937 36 Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?EBI University of South Australia
29459274 69 Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.EBI Shanghai HaiHe Pharmaceutical, Co. Ltd
28987604 3 Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro.EBI China Pharmaceutical University
29550093 13 Discovery of novel CDK inhibitors via scaffold hopping from CAN508.EBI Chinese Academy of Medical Sciences and Peking Union Medical College
29329658 63 Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.EBI Semmelweis University
29273417 26 An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold.EBI University of KwaZulu-Natal
29778892 48 Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors.EBI University of Tours
30067358 79 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 Company Limited
29853338 31 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
29853332 50 Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.EBI Universit£ de Nantes
28651979 6 Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate.EBI Nankai University
29370702 41 Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.EBI CSIR-Indian Institute of Integrative Medicine
28947155 34 Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.EBI Sanofi Genzyme
28830649 101 Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.EBI Genentech
28827110 54 Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors.EBI Korea Research Institute of Chemical Technology
27721154 660 Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.EBI University of Paris
29144137 60 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
28302507 124 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 Co., Ltd
29518312 78 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
28487075 36 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
9650799 159 [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.BDB Novartis Pharma AG
19115845 39 First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.BDB Nerviano Medical Sciences srl
19128055 24 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
19007108 32 Synthetic and Crystallographic Studies of a New Inhibitor Series Targeting Bacillus anthracis Dihydrofolate Reductase.BDB University of Connecticut
17228885 10 New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.BDB Universita di Pisa
17064068 36 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB Palacky University
15261277 30 Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.BDB Cyclacel Limited