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197 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28279846 36 Design, synthesis, and biological evaluation of novel 4-anilinoquinazoline derivatives bearing amino acid moiety as potential EGFR kinase inhibitors.EBI Xuzhou Medical University
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI Abbvie Bioresearch Center
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck
27884697 65 3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization.EBI Cxs
27573544 43 Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.EBI Taiwan National Health Research Institutes
27391133 76 Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening.EBI University Of Berne
27774127 75 Discovery of a Series of 5,11-Dihydro-6EBI Dana-Farber Cancer Institute
27335255 33 Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.EBI Entremed
27209235 8 Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors.EBI Sookmyung Women'S University
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
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
27041399 32 Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors.EBI Ewha Womans University
26890118 8 Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties.EBI Mendeleyev University Of Chemical Technology
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
26614408 106 Identification of azabenzimidazoles as potent JAK1 selective inhibitors.EBI Astrazeneca
26384287 65 Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.EBI Kangwon National University
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26320624 45 Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.EBI Novartis Institutes For Biomedical Research
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
26048792 4 Identification of 3,5,6-substituted indolin-2-one's inhibitors of Aurora B by development of a luminescent kinase assay.EBI Chinese Academy Of Medical Sciences And Peking Union Medical College
25262942 189 Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI Astrazeneca
25007344 73 Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.EBI Christian-Albrechts-University Of Kiel
26101564 20 MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.EBI Takeda Pharmaceutical
25812967 6 Synthesis and biological evaluation of 2,4-diaminopyrimidines as selective Aurora A kinase inhibitors.EBI Lanzhou University
25791677 15 Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.EBI Zhengzhou University
25766633 9 Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor.EBI The University Of Michigan Medical School
25369539 116 SAR156497, an exquisitely selective inhibitor of aurora kinases.EBI Sanofi
25089810 79 Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.EBI National Taiwan 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
25042560 18 Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors.EBI Ewha Womans University
25036791 56 Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.EBI National Taiwan University
25022204 78 Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.EBI Universit£
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
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
25456085 4 Synthesis and biological evaluation of novel oxindole-based RTK inhibitors as anti-cancer agents.EBI Wenzhou Medical University
25383627 85 Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.EBI Genentech
25270403 44 Discovery of 4-aminoquinazoline--urea derivatives as Aurora kinase inhibitors with antiproliferative activity.EBI Southeast 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
24773549 20 Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.EBI Development Center For Biotechnology
24681066 35 Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.EBI Sun Yat-Sen University
24462666 105 Discovery of 6-aryl-azabenzimidaoles that inhibit the TBK1/IKK-e kinases.EBI Astrazeneca
23906342 14 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.EBI Takeda Pharmaceutical
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
24195668 57 Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.EBI The Institute Of Cancer Research
24100158 148 Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI Nerviano Medical Sciences
24900590 55 Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.EBI Glaxosmithkline
24044867 86 Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI Califia Bio
23856049 50 Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: optimization of kinase selectivity and pharmacokinetics.EBI Osi Pharmaceuticals
23829549 145 The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.EBI Entremed
23773865 49 Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.EBI Osi Pharmaceuticals
23707920 3 A thienopyrimidine derivative induces growth inhibition and apoptosis in human cancer cell lines via inhibiting Aurora B kinase activity.EBI Fudan University
23808327 29 Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor.EBI National Health Research Institutes
23664099 32 Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.EBI Xuzhou Medical College
23570792 61 SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.EBI Emd-Serono Research Institute
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical
23434140 35 Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI East China University Of Science And Technology
23414845 44 Structure-based discovery of cellular-active allosteric inhibitors of FAK.EBI Takeda Pharmaceutical
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
21903390 79 Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.EBI Glaxosmithkline
19349179 47 4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.EBI Glaxosmithkline
23099093 84 Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases.EBI Mrc Technology
23043539 60 Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.EBI The Institute Of Cancer Research
22883026 34 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.EBI Takeda Pharmaceutical
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
22920039 9 Crystal structure of human aurora B in complex with INCENP and VX-680.EBI University Of Oxford
22827572 67 Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).EBI Glaxosmithkline
22380736 90 Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.EBI Ambit Biosciences
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
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
22695126 98 Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.EBI Abbott Laboratories
22727637 85 Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI Abbott Laboratories
22632936 42 Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.EBI Myrexis
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
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
22607669 45 Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.EBI Biogen Idec
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen
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
22247788 40 Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.EBI TBA
22503250 128 Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.EBI Amri
22465635 95 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI Abbott Laboratories
22326168 67 Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.EBI Biogen Idec
22305584 145 Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKe kinases.EBI Astrazeneca R&D Boston
21128645 60 Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.EBI Evotec (Uk)
21128646 88 Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.EBI Merck Research Laboratories
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20570526 84 Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.EBI National Taiwan University
20565112 55 Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.EBI The Institute Of Cancer Research
20420387 118 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI Glaxosmithkline
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
20038108 19 Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.EBI Wyeth Research
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
19320489 125 Discovery and development of aurora kinase inhibitors as anticancer agents.EBI Vertex Pharmaceuticals
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
17360485 10 Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.EBI Millennium Pharmaceuticals
18324761 65 Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.EBI Amgen
18324759 133 Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.EBI Amgen
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University Of Oxford
18243698 11 Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.EBI National Health Research Institutes
16451062 46 Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI Astrazeneca
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
22153662 137 Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.EBI Astrazeneca
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
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
21982797 128 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.EBI Peking University
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21855335 185 Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.EBI Merck Research Laboratories
21802948 125 Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.EBI Ambit Biosciences
21741249 32 Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.EBI Heinrich Heine Universit£T
20674350 63 Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
20573509 23 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.EBI Mitsubishi Tanabe Pharma
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
21341675 266 Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI Glaxosmithkline
24900229 41 Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI TBA
21288717 131 Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.EBI Abbott Laboratories
21282054 178 Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.EBI Abbott Laboratories
20965724 57 Identification of potent ITK inhibitors through focused compound library design including structural information.EBI Nycomed
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
20833547 19 Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.EBI The Institute Of Cancer Research
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
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
16783341 34 Rational design of inhibitors that bind to inactive kinase conformations.EBI Novartis Research Foundation
20681538 61 Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.EBI Development Center For Biotechnology
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel
20459125 60 Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.EBI Amgen
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
19894727 164 Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.EBI Wyeth Research
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
20338758 39 Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors.EBI S*Bio
20335034 7 Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.EBI Glaxosmithkline
20223663 100 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.EBI Wyeth Research
20188552 75 Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI Wyeth Research
20167481 66 Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.EBI Sanofi-Aventis
19854649 49 Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI Wyeth Research
19854645 87 Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI Wyeth Research
19646866 35 2-Aminobenzimidazoles as potent Aurora kinase inhibitors.EBI Sunesis Pharmaceuticals
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences
20097074 5 New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.EBI Schering-Plough Research Institute
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19692247 295 Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.EBI 4Sc
19857966 62 Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.EBI Astrazeneca R&D Boston
19888761 52 Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.EBI Hanmi Research Center
19447622 128 The discovery of the potent aurora inhibitor MK-0457 (VX-680).EBI Vertex Pharmaceuticals
19364658 113 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Wyeth Research
19211246 320 N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.EBI 4Sc
19101143 70 Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).EBI Glaxosmithkline
19062275 39 Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.EBI Amgen
19035792 85 Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI Glaxosmithkline
18682324 33 Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI Amgen
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
18529047 156 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.EBI Eberhard-Karls University
18524423 16 Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.EBI Eberhard-Karls University
17933533 36 Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.EBI The Institute Of Cancer Research
17665890 60 An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.EBI University Of Athens
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
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen
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
27450574 3 Structure-based virtual screening toward the discovery of novel inhibitors of the DNA repair activity of the human apurinic/apyrimidinic endonuclease 1.BDB Universidade De Lisboa
10353842 147 Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R).BDB National Institute Of Diabetes And Digestive And Kidney Diseases
9650799 159 [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.BDB Novartis Pharma
7890738 3 Expression of recombinant homo-oligomeric 5-hydroxytryptamine3 receptors provides new insights into their maturation and structure.BDB Medical Research Council Centre
19807733 6 Active site ring-opening of a thiirane moiety and picomolar inhibition of gelatinases.BDB University Of Notre Dame
19703036 15 Antiproliferative activity against MCF-7 breast cancer cells by diamino-triazaspirodiene antifolates.BDB National University Of Singapore
6266565 14 The binding of [3H]-prostacyclin to membranes of a neuronal somatic hybrid.BDB Royal Postgraduate Medical School
17630989 9 Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.BDB Abbott Laboratories
21513882 3 Sequential mechanism of assembly of multidrug efflux pump AcrAB-TolC.BDB University Of Oklahoma
18849972 45 Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.BDB The Scripps Research Institute
19877603 51 Identification and Biological Evaluation of a Series of 1H-Benzo[de]isoquinoline-1,3(2H)-diones as Hepatitis C Virus NS5B Polymerase Inhibitors.BDB Irbm, Mrl Rome
15974572 14 Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.BDB Vernalis (R&D)
15723556 4 Use of binding enthalpy to drive an allosteric transition.BDB University Of Maryland