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218 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27987485 74 Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors.EBI Hamdard University
28092860 36 Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.EBI Peking University
27769032 3 Design of a doxorubicin-peptidomimetic conjugate that targets HER2-positive cancer cells.EBI University of Louisiana at Monroe
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27769671 66 Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.EBI Tsinghua University
27769623 21 Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Ocean University of China
27491023 286 Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.EBI University of Auckland
27187856 43 Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.EBI China Pharmaceutical University
27348537 60 Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.EBI East China University of Science& Technology
27132165 29 Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.EBI Southern Medical University
27131066 36 An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Chinese Academy of Sciences
27387355 32 6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR.EBI Zhejiang University
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
27288180 83 Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.EBI Harvard Medical School
27190603 73 Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.EBI AstraZeneca
27173802 2 Sequential one-pot synthesis of bis(indolyl)glyoxylamides: Evaluation of antibacterial and anticancer activities.EBI Birla Institute of Technology and Science
27010810 24 Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.EBI OriBase Pharma
27234887 84 Discovery of new [1,4]dioxino[2,3-f]quinazoline-based inhibitors of EGFR including the T790M/L858R mutant.EBI Beijing University of Technology
27131639 26 Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors.EBI Fudan University
27106711 87 Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).EBI Green Valley Research Institute
27106709 92 Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.EBI Korea Research Institute of Chemical Technology
26968253 24 Recent progress on third generation covalent EGFR inhibitors.EBI Pfizer Inc.
26756222 70 Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.EBI Pfizer Inc.
26819674 66 Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.EBI Genentech
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
26879314 26 Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors.EBI Beijing University of Technology
26829280 26 Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.EBI Dalian Medical University
26698536 56 Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EBI Chinese Academy of Sciences
26639762 55 4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.EBI Genentech
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
26652482 64 Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.EBI Nanjing University
26475520 43 Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.EBI Korea University of Science and Technology (UST)
26396685 19 Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.EBI Amgen Inc.
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26313252 22 Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.EBI AstraZeneca
25172421 26 Design, synthesis and molecular modeling of biquinoline-pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors.EBI Nanjing University
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
26071372 89 Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI Astellas Pharma Inc.
25975640 60 Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.EBI Technische Universit£t Dortmund
25827399 52 Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.EBI Chinese Academy of Sciences
25794791 13 Recent advances in the chemistry and biology of pyridopyrimidines.EBI Universit£ d'Orl£ans
25619636 4 Computer-aided identification of novel anticancer compounds with a possible dual HER1/HER2 inhibition mechanism.EBI Cardiff University
25409491 83 A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI Zhejiang University
25383627 85 Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.EBI Genentech Inc.
25305330 75 Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.EBI Southeast University
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
24915291 73 Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.EBI Peking University
24900886 66 Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.EBI Chinese Academy of Sciences
24565969 69 Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.EBI Chinese Academy of Sciences
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical Co., Ltd
23414845 44 Structure-based discovery of cellular-active allosteric inhibitors of FAK.EBI Takeda Pharmaceutical Company 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
23107515 3 Fluorescence study for selecting specific ligands toward HER2 receptor: an example of receptor fragment approach.EBI Institute of Biostructures and Bioimages
23391364 78 Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.EBI Nanjing University
23245802 7 Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives containing benzodioxole as potential anticancer agents.EBI Nanjing University
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
14561085 94 Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.EBI University of Tennessee Health Sciences Center
22621397 39 Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI Covalution Pharma BV
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
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
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
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
23039927 44 Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.EBI Martin-Luther University Halle-Wittenberg
23025996 4 Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents.EBI Nanjing 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
22901387 18 Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors.EBI Nanjing University
22868229 2 A fluorescent reporter of ATP binding-competent receptor kinases.EBI University of Miami
22863529 31 Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.EBI Chinese Academy of Sciences
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
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
22280453 19 Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides.EBI Universit£ degli Studi di Parma
20594859 40 Synthesis, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents.EBI Nanjing University
20570525 56 Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.EBI Chinese Academy of Sciences
19635666 119 Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.EBI Incyte Corporation
19821562 34 Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.EBI Bristol-Myers Squibb Research and Development
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
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
19017562 45 Discovery and development of heat shock protein 90 inhibitors.EBI Memorial Sloan-Kettering Cancer Center
19111461 50 Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.EBI GlaxoSmithKline
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18395443 37 Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.EBI Bristol-Myers Squibb
18508264 44 Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.EBI Johnson& Johnson Pharmaceutical Research& Development
18343125 9 Formation of fluorine-18 labeled diaryl ureas--labeled VEGFR-2/PDGFR dual inhibitors as molecular imaging agents for angiogenesis.EBI Hadassah Hebrew University Hospital
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18182285 48 Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.EBI AstraZeneca
18061446 35 A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.EBI Centre de Recherches
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
16279804 40 Anilinodialkoxyquinazolines: screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes.EBI Lawrence Berkeley National Laboratory
16777410 50 Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.EBI GlaxoSmithKline
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
15715478 164 Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.EBI Wyeth Research
12502359 70 Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).EBI Wyeth Research
12270171 14 Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.EBI Wyeth Research
 1 Indolocarbazoles. 1. Total synthesis and protein kinase inhibiting characteristics of compounds related to K-252c.EBI TBA
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
22361272 74 Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors.EBI Nanjing University
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
22169262 26 Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.EBI Shenyang Pharmaceutical University
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
22182581 36 Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.EBI East China University of Science and Technology
22169601 16 Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.EBI University of Regensburg
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
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
21920766 64 Metronidazole acid acyl sulfonamide: a novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors.EBI Nanjing University
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.
21665484 37 Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.EBI Chinese Academy of Sciences
21705217 60 Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI Bristol-Myers Squibb
21561771 39 Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical Co. Ltd.
21405128 47 Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.EBI Chinese Academy of Sciences
21334203 62 Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.EBI Shionogi& Co., Ltd
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21177105 38 Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Research and Development
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
20817523 61 Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.EBI Abbott Laboratories
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
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
19483697 23 Phage-encoded combinatorial chemical libraries based on bicyclic peptides.EBI Laboratory of Molecular Biology, Medical Research Council
18559524 21 BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI Boehringer Ingelheim Austria GmbH
20466555 2 Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.EBI Southeast University
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical 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
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
19815412 34 Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.EBI Shanghai Hengrui Pharmaceuticals Co., Ltd.
20031417 40 Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.EBI Hadassah Hebrew University Hospital
20005116 42 Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.EBI Nanjing University
19914837 74 Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas as antitumor agents.EBI Nanjing University
19914835 50 Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.EBI Nanjing University
20143778 70 Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.EBI Curis Inc
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 AG
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
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.
18842405 34 Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.EBI GlaxoSmithKline Research& Development
 15 Inhibition of the her2 tyrosine kinase and characterization of a hydrophobic site near the nucleotide binding domainEBI TBA
19457660 90 Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.EBI Incyte Corporation
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
18818075 25 The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.EBI GlaxoSmithKline
18678484 57 A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.EBI Johnson & Johnson Pharmaceutical Research and Development
18667312 24 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.EBI The Scripps Research Institute
18653333 32 4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development
18610999 24 Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.EBI Institute of Materia Medica
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
18500794 25 Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.EBI University of Southern California
17981366 9 Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.EBI Freie Universität Berlin
18313293 26 Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.EBI Centre de Recherches
18289854 44 Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.EBI Bristol-Myers Squibb Research and Development
17869514 20 Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.EBI AstraZeneca
17606372 66 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17574416 39 Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17532631 105 Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17398092 74 The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.EBI Pfizer, Inc.
17368025 42 Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17270437 68 New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17256836 84 Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.EBI Incyte Corporation
17174554 12 Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.EBI Sun Yat-sen University
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.
16789733 41 Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16759097 36 The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR).EBI McGill University Health Center/ Royal Victoria Hospital
16530412 13 High-throughput screening for Hsp90 ATPase inhibitors.EBI The University of Kansas
16483772 52 Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.EBI GlaxoSmithKline
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
16249085 26 Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.EBI Novartis Institutes for BioMedical Research
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
16111887 104 New dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16078851 47 High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.EBI Hadassah Hebrew University
16055332 18 5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.EBI AstraZeneca
15993060 10 Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.EBI GlaxoSmithKline
15943473 136 Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
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
15546730 9 Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15317463 16 Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15177482 90 Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI Novartis Institutes for BioMedical Research
14592495 60 Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12825933 17 Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.EBI Institut für molekulare Physiologie
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12086485 10 Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.EBI Boehringer Ingelheim Pharmaceuticals
12039561 30 Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.EBI Bayer Research Center
11472210 9 Disabling erbB receptors with rationally designed exocyclic mimetics of antibodies: structure-function analysis.EBI University of Pennsylvania School of Medicine
11378364 34 Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.EBI Research Biomet. Glaxo Wellcome Medicines Research Centre
10753475 61 Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.EBI University of Auckland
10464027 118 Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.EBI University of Oregon
10346932 53 Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.EBI University of Auckland
9651163 268 Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.EBI SUGEN, Inc.
9089334 3 Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases.EBI Warner-Lambert Company
8064792 25 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.EBI Sterling Winthrop Pharmaceuticals Research Division
7902440 104 Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins.EBI Hebrew University of Jerusalem
24634223 8 Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein.BDB University of Toronto
19434638 66 Synthesis and in vitro activity of heterocyclic inhibitors of CYP2A6 and CYP2A13, two cytochrome P450 enzymes present in the respiratory tract.BDB University of Basel
19199329 10 Crystal structure analysis and in silico pKa calculations suggest strong pKa shifts of ligands as driving force for high-affinity binding to TGT.BDB Philipps-Universität Marburg
18921992 9 Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.BDB Pfizer
17539621 17 Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.BDB Universita degli Studi
17560788 15 Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.BDB Pfizer
17343373 54 Carbonic anhydrase inhibitors: inhibition of isozymes I, II, and IX with triazole-linked O-glycosides of benzene sulfonamides.BDB Griffith University
17275837 4 A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera.BDB Astex
16962773 8 Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.BDB University of Michigan
11033082 16 Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.BDB SmithKline Beecham Pharmaceuticals
10395478 126 Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.BDB University of Auckland