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176 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
28109791 44 Identification of a selective inhibitor of transforming growth factor▀-activated kinase 1 by biosensor-based screening of focused libraries.EBI Chugai Pharmaceutical Co., Ltd.
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27527804 109 Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).EBI Teva Branded Pharmaceutical Products R&D
27144831 149 Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.EBI ARIAD Pharmaceuticals, Inc.
27288183 130 Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI Southeast 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 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
27106709 92 Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.EBI Korea Research Institute of Chemical Technology
26951750 59 Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for Biomedical Research
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
26235945 58 Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.EBI Korea Research Institute of Chemical Technology
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
26005534 158 (R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.EBI Genomics Institute of the Novartis Research Foundation
25559205 31 Cyclopentyl-pyrimidine based analogues as novel and potent IGF-1R inhibitor.EBI Piramal Enterprises Limited
25180654 29 Design, synthesis, and evaluation of novel imidazo[1,2-a][1,3,5]triazines and their derivatives as focal adhesion kinase inhibitors with antitumor activity.EBI Universit£ Paris Descartes
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
25271963 93 Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.EBI AstraZeneca
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24900877 107 Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.EBI Merck Research Laboratories
24685542 67 Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI Bristol-Myers Squibb Research and Development
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 Company Limited
24157370 22 The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.EBI Chugai Pharmaceutical Co., Ltd
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.
24044867 86 Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI Califia Bio Inc.
23755884 23 Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.EBI Takeda Pharmaceutical Company, Ltd
23742252 81 Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase EBI Genomics Institute of the Novartis Research Foundation
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical Co., Ltd
23249297 75 Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI Heinrich-Heine University
23312943 166 Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
22765894 223 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.EBI Exelixis
22612866 123 Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.EBI AstraZeneca
23123015 22 Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.EBI Takeda Pharmaceutical Company Limited
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 Company Limited
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
22734674 81 The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.EBI Amgen Inc.
22141319 56 Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.EBI Cephalon, Inc.
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 Co. Ltd
22795331 51 Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.EBI Janssen Pharmaceutical Companies of Johnson& Johnson
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
24900237 41 Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.EBI TBA
22372864 25 Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.EBI Hanmi Research Center
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen Inc.
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
24900346 90 Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI TBA
21441024 74 Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.EBI Sanofi-aventis
21123062 48 Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.EBI Cephalon, Inc
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20153646 28 Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.EBI Institute of Science and Technology
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
19716697 110 The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.EBI Boehringer Ingelheim Pharmaceuticals
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
19610618 41 Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.EBI University of South Florida
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute
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
19081716 57 Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.EBI GlaxoSmithKline
9677190 49 Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI University of California
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer Global Researchand Development
18321716 7 ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.EBI Institute of Molecular Physiology
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
17983756 55 Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI OSI Pharmaceuticals, Inc.
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
17887663 34 Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.EBI Pfizer Global Research and Development
16480284 126 Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.EBI Pfizer Global Research and Development
12166950 208 Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI Millennium Pharmaceuticals, Inc.
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
22310227 89 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI GlaxoSmithKline
16476733 18 Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.EBI University of Queensland
22269278 50 Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.EBI Chugai Pharmaceutical Co., Ltd.
22285571 49 QSAR studies for prediction of cross-ß sheet aggregate binding affinity and selectivity.EBI The Ohio State University College of Medicine
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
21967808 52 Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.EBI Cephalon, Inc.
22169263 73 Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.EBI Cephalon, Inc.
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
22119469 107 Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI Pfizer Inc.
22101132 41 Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.EBI Shionogi& Co., Ltd
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
22061645 68 Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.EBI Cephalon, Inc.
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
21859094 61 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.EBI Cephalon, Inc.
21823617 58 9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical Co., Ltd.
21812414 106 Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).EBI Pfizer Inc.
21775140 69 Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.EBI AstraZeneca
21708465 141 Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.EBI St. Jude Children's Research Hospital
21632243 48 Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.EBI Cephalon, Inc.
21561767 48 Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI ARIAD Pharmaceuticals, Inc.
21493067 22 In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.EBI AstraZeneca R&D Boston
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
21391610 139 Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI Vertex Pharmaceuticals (Europe) Ltd.
21353551 23 Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.EBI OSI Pharmaceuticals, Inc
21414779 64 Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.EBI Amgen Inc.
24900240 19 Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.EBI TBA
24900229 41 Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI TBA
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21074994 46 Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.EBI Cephalon, Inc
21190849 53 2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.EBI Cephalon, Inc.
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
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
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
20833055 44 Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.EBI Takeda Pharmaceutical Co., Ltd
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
18559524 21 BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI Boehringer Ingelheim Austria GmbH
17376430 19 ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents.EBI The Hebrew University of Jerusalem
20472447 45 Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).EBI Nycomed Pharma Pvt. Ltd
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
20430619 73 8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.EBI Cephalon, Inc.
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
20382527 26 Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.EBI Bristol-Myers Squibb Research and Development
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
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI CGI Pharmaceuticals, Inc.
19854052 420 Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.EBI Genomics Institute of the Novartis Research Foundation (GNF)
20178321 74 Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.EBI Chinese Academy of Sciences
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences Srl
20121196 12 Discovery of novel fibroblast growth factor receptor 1 kinase inhibitors by structure-based virtual screening.EBI Yale University
20093027 92 Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI Chugai Pharmaceutical Co, Ltd
19775160 79 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.EBI Takeda Pharmaceutical Company, Ltd.
19362847 51 Design and synthesis of a novel tyrosine kinase inhibitor template.EBI St Jude Children's Research Hospital
1479375 215 Protein-Tyrosine Kinase Inhibition: Mechanism-Based Discovery of Antitumor AgentsEBI TBA
 42 A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylationEBI TBA
 99 Discovery and structure-activity studies of a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitorsEBI TBA
19327989 40 Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI Pfizer Global R&D
19317452 155 Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.EBI Wyeth Research
19246196 104 5-Aminomethylbenzimidazoles as potent ITK antagonists.EBI Boehringer Ingelheim Pharmaceuticals Inc.
19211246 320 N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.EBI 4SC AG
19101143 70 Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).EBI GlaxoSmithKline
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
19035792 85 Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI GlaxoSmithKline
18819799 72 Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).EBI Johnson & Johnson
18819794 53 Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.EBI Johnson & Johnson
18793846 33 Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.EBI Genomics Institute of the Novartis Research Foundation (GNF)
18691885 60 Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.EBI ARIAD Pharmaceuticals, Inc.
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
17185414 30 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI Genomics Institute of the Novartis Research Foundation
18308565 70 Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.EBI Cephalon, Inc.
18289854 44 Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.EBI Bristol-Myers Squibb Research and Development
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
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
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16451066 58 Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase.EBI ChemBridge Research Laboratories and ChemBridge Corporation
16366598 51 (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.EBI Johnson & Johnson Pharmaceutical Research and Development
16198560 19 Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.EBI ImClone Systems Inc
16134929 22 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.EBI Bristol-Myers Squibb Co
15771417 48 2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development
15711537 653 A small molecule-kinase interaction map for clinical kinase inhibitors.EBI Ambit Biosciences
15615512 21 Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
14640546 46 A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinEBI Cephalon, Inc
12941342 21 Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.EBI Aventis Pharmaceuticals
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12039590 51 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
11000003 8 Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.EBI Merck Research Laboratories
9240345 33 Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.EBI Parke-Davis Pharmaceutical Research
2033582 2 Phosphonate-containing inhibitors of tyrosine-specific protein kinases.EBI National Cancer Institute
27231830 27 Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.BDB AIMST University
25346162 16 Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO-B Inhibitors.BDB Pontificia Universidad Catˇlica de Chile
19743875 5 Characterization of the CHK1 allosteric inhibitor binding site.BDB Pfizer
21848665 9 Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands.BDB Yeditepe University
7681406 8 Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors.BDB Sanofi Recherche
11567092 4 Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.BDB GSK
16495061 8 Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.BDB Johnson & Johnson Pharmaceutical
16690314 13 BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.BDB Merck Research Laboratories