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145 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28169164 19 Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors.EBI Takeda California
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.
27592392 12 Identification of acylthiourea derivatives as potent Plk1 PBD inhibitors.EBI Peking University
27624074 25 Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain.EBI National Cancer Institute
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's University
27017542 7 Small molecules that target phosphorylation dependent protein-protein interaction.EBI RIKEN
26881908 13 De Novo Design at the Edge of Chaos.EBI Swiss Federal Institute of Technology (ETH)
27055065 92 Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.EBI The Institute of Cancer Research
27003761 120 Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.EBI Nerviano Medical Sciences Srl
27117263 51 Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC┐ inhibitors.EBI Takeda Pharmaceutical Company, Ltd
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26762835 342 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).EBI Icahn School of Medicine at Mount Sinai
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26318067 34 Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI Hanyang University
26191363 29 BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.EBI University of Maryland
26222319 192 Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.EBI Nerviano Medical Sciences Srl
25007344 73 Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor▀ (PDGF-R▀) guided by water thermodynamics.EBI Christian-Albrechts-University of Kiel
25791677 15 Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.EBI Zhengzhou University
25827523 275 Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI Vertex Pharmaceuticals Inc.
25556101 18 Identification of indole-3-carboxylic acids as non-ATP-competitive Polo-like kinase 1 (Plk1) inhibitors.EBI China Pharmaceutical University
25043312 104 Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.EBI University Health Network
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24867403 156 The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.EBI EntreMed Inc.
25462247 20 In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI Fudan University
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24859762 10 Aromatic diacylhydrazine derivatives as a new class of polo-like kinase 1 (PLK1) inhibitors.EBI Nanjing University
24479418 39 Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.EBI Heinrich-Heine-Universit£t
24256217 177 Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).EBI The Institute of Cancer Research
24328302 94 Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.EBI Heinrich-Heine-Universit£t D£sseldorf
24100158 148 Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI Nerviano Medical Sciences S.r.l.
23829549 145 The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.EBI EntreMed Inc.
23522834 72 Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.EBI Elan Pharmaceuticals
23664874 16 Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).EBI Takeda California
23634759 32 Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125).EBI Shionogi Pharmaceutical Research Center
23498919 7 Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1.EBI Korea Basic Science Institute
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical Co., Ltd
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis
23362959 72 Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.EBI Sichuan University
23249297 75 Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI Heinrich-Heine University
23276450 6 Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.EBI The University of Tokyo
19303774 87 1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI GlaxoSmithKline R&D
17194588 92 N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI GlaxoSmithKline R&D
22621397 39 Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI Covalution Pharma BV
23159568 8 Non-proteinogenic amino acids in the pThr-2 position of a pentamer peptide that confer high binding affinity for the polo box domain (PBD) of polo-like kinase 1 (Plk1).EBI Frederick National Laboratory for Cancer Research
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
23116168 42 Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.EBI Sichuan University
22980219 55 Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.EBI Takeda Pharmaceutical Co. Ltd
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
22632936 42 Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.EBI Myrexis Inc.
22452518 22 Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.EBI Sichuan University
22439974 79 Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.EBI Takeda Pharmaceutical Company Limited
22404346 52 Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.EBI The Institute of Cancer Research
22560627 70 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.EBI Technische Universit£t Braunschweig
22168626 32 Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.EBI Ambit Biosciences
21353571 26 Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI Hanyang University
20932759 100 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.EBI Nerviano Medical Sciences srl
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20000735 12 Through the"gatekeeper door": exploiting the active kinase conformation.EBI Nerviano Medical Sciences
20138514 93 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI Vertex Pharmaceuticals Inc
20138512 82 Discovery of potent and bioavailable GSK-3beta inhibitors.EBI Roche Palo Alto
20000469 179 Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.EBI Boehringer Ingelheim Pharmaceuticals
20170163 157 Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation.EBI Technische Universitat Braunschweig
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
17850214 99 The selectivity of protein kinase inhibitors: a further update.EBI University of Dundee
19522465 102 Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).EBI Boehringer Ingelheim Pharma GmbH&Co KG
18789685 172 Kinase array design, back to front: biaryl amides.EBI GlaxoSmithKline R&D
17360485 10 Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.EBI Millennium Pharmaceuticals Inc.
18362070 79 Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
16451062 46 Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI Centre de Recherches
22377675 44 Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.EBI Westf£lische Wilhelms-Universit£t M£nster
17018693 30 Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI GlaxoSmithKline Pharmaceuticals Inc.
16249345 25 Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI GlaxoSmithKline
22136433 67 7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.EBI Ludwig-Maximilians University of Munich
22154349 123 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences srl
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
22003817 71 Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.EBI Takeda Pharmaceutical Company Limited
21982797 128 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.EBI Peking University
22014755 36 Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI Hanyang University
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21936542 143 Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI Novartis Institute for BioMedical Research
21741249 32 Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.EBI Heinrich-Heine-Universit£t
21778054 3 Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1.EBI Helmholtz Center Dresden-Rossendorf
21723120 100 Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.EBI Nerviano Medical Sciences srl
21627121 22 Irreversible Nek2 kinase inhibitors with cellular activity.EBI University of California
21470862 110 NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI Nerviano Medical Sciences srl
21366329 29 Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.EBI Institute of Cancer Research
21080629 153 Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.EBI University of Regensburg
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
21035334 55 Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.EBI Martin Luther University Halle-Wittenberg
20965724 57 Identification of potent ITK inhibitors through focused compound library design including structural information.EBI Nycomed GmbH
20936789 56 Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization.EBI Institute of Cancer Research
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences Srl
20817473 57 Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI Nerviano Medical Sciences-Oncology
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc.
20188579 42 Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.EBI Temple University School of Medicine
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
17028580 2 Probing cell-division phenotype space and Polo-like kinase function using small molecules.EBI Rockefeller University
20594842 90 Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.EBI GlaxoSmithKline
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel Ltd.
20397705 208 Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences Srl
20346655 117 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.EBI Abbott Laboratories
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
19864136 45 Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.EBI Wyeth Research
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences Srl
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19589677 65 Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors.EBI Banyu Tsukuba Research Institute
19414255 58 Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI Vertex Pharmaceuticals Inc
19097792 24 Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.EBI AstraZeneca R&D Boston
19053831 39 Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.EBI Institute of General Genetics
18929484 26 Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.EBI GlaxoSmithKline
18762425 42 Pharmacophore modeling and virtual screening for designing potential PLK1 inhibitors.EBI Sichuan University
17135248 7 Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects.EBI ActivX Biosciences, Inc.
17658776 109 Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI Abbott Laboratories
17149885 20 Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.EBI Eberhard Karls University
17027260 41 Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.EBI GlaxoSmithKline K.K.
16216502 119 Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.EBI Abbott Laboratories
18829454 12 Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.BDB University of Pittsburgh
19359241 26 Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.BDB University of Manchester
22570300 3 Peptoid-Peptide hybrid ligands targeting the polo box domain of polo-like kinase 1.BDB Frederick National Lab
21765407 30 Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.BDB National Cancer Institute-Frederick
17028581 3 Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance.BDB University of Cambridge
19237286 30 Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.BDB GSK
19097784 55 Discovery of thiophene inhibitors of polo-like kinase.BDB GSK
16997559 29 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase.BDB GSK
18005335 12 Selectivity-determining residues in Plk1.BDB Pfizer
18793847 33 Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.BDB Sunesis Pharmaceuticals
17655330 84 Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.BDB Abbott Laboratories
17040210 10 BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.BDB University of Dundee
18790636 22 Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.BDB Sunesis Pharmaceuticals