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127 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's University
27187860 18 Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.EBI Yonsei 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
26717201 68 Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.EBI Shenyang Pharmaceutical University
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
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.
25791677 15 Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.EBI Zhengzhou University
25723005 111 The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.EBI TBA
25369539 116 SAR156497, an exquisitely selective inhibitor of aurora kinases.EBI Sanofi
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
22929232 89 Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.EBI Amgen Inc.
17293140 160 3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.EBI Dalian University
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
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
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
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
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
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.
22406116 4 Discovery of loperamide as an antagonist of angiopoietin1 and angiopoietin2 by virtual screening.EBI Zhejiang Gongshang University
22148921 48 Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-cEBI Cephalon, Inc.
20420387 118 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI GlaxoSmithKline
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18324759 133 Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.EBI Amgen Inc.
18311900 89 Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.EBI Amgen Inc.
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18343109 51 TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.EBI Cephalon, Inc.
18278858 93 Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen Inc.
18083554 54 N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.EBI Amgen Inc.
16876403 85 Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
12477352 85 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.EBI Novartis Pharma AG
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
22221201 32 VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.EBI University of Kentucky
16249345 25 Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI GlaxoSmithKline
22169262 26 Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.EBI Shenyang Pharmaceutical University
22014550 337 Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI Ansaris
22003817 71 Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.EBI Takeda Pharmaceutical Company Limited
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
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.
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer 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.
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.
21414779 64 Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.EBI Amgen Inc.
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
20961062 42 Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.EBI Pfizer Inc.
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
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc.
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
19039322 50 Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.EBI Center for Molecular Medicine of the Austrian Academy of Sciences
16783341 34 Rational design of inhibitors that bind to inactive kinase conformations.EBI Novartis Research Foundation
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
20459125 60 Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.EBI Amgen Inc.
20430619 73 8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors.EBI Cephalon, Inc.
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.
19854647 17 Novel thienopyrimidine and thiazolopyrimidine kinase inhibitors with activity against Tie-2 in vitro and in vivo.EBI AstraZeneca
20031417 40 Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.EBI Hadassah Hebrew University Hospital
19692247 295 Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.EBI 4SC AG
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.
19361991 80 Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI Vertex Pharmaceuticals Inc
19211246 320 N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.EBI 4SC AG
19062275 39 Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.EBI Amgen Inc.
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
18993068 75 Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.EBI Amgen Inc.
18818075 25 The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.EBI GlaxoSmithKline
18723346 26 Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.EBI Amgen Inc.
18682324 33 Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI Amgen, Inc.
18676144 93 Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.EBI AstraZeneca
18602262 56 Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI GlaxoSmithKline R&D
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
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.
18248988 16 Entry into a new class of protein kinase inhibitors by pseudo ring design.EBI Novartis Institutes for BioMedical Research
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
17618114 11 Pyridinylimidazole inhibitors of Tie2 kinase.EBI GlaxoSmithKline
17425296 161 1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.EBI Abbott Laboratories
17391959 100 Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
17350837 59 Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.EBI Amgen Inc.
17343372 143 Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.EBI Abbott Laboratories
17280833 52 Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.EBI Amgen Inc.
17239587 43 1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.EBI Cephalon Inc.
17234410 82 Discovery of thienopyridines as Src-family selective Lck inhibitors.EBI Abbott Bioresearch Center
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.
16931012 61 Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.EBI TargeGen, Inc.
16890434 64 Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.EBI Cephalon, Inc.
16759855 130 1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
16750628 47 Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.EBI Abbott Laboratories
16735117 50 Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.EBI Abbott Laboratories
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
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
15109663 26 A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.EBI Abbott Bioresearch Center
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
12825933 17 Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.EBI Institut für molekulare Physiologie
12039590 50 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
11934592 20 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
11012022 92 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.EBI BASF Bioresearch Corporation
11012021 59 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI BASF Bioresearch Corporation
16492761 51 An efficient rapid system for profiling the cellular activities of molecular libraries.BDB Genomics Institute of the Novartis Research Foundation
19199284 24 Development and biological evaluation of a novel aurora A kinase inhibitor.BDB Parc de Recerca Biomedica de Barcelona
15696596 33 Inhibition of angiogenesis-relevant receptor tyrosine kinases by sulindac analogues.BDB Max-Planck-Institut für Molekulare Physiologie
19764794 60 Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.BDB Amgen
18321037 129 Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.BDB Amgen
18260617 131 3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.BDB Abbott Laboratories
17676829 78 Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors.BDB GSK
16884310 97 Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.BDB Amgen
17696416 45 Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.BDB Amgen
17276055 17 Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.BDB GlaxoSmithKline
17253678 70 Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.BDB Amgen
17253679 69 Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.BDB Amgen
16162008 146 Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.BDB Abbott Laboratories
12039591 63 Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.BDB Abbott Bioresearch Center
15837294 36 Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.BDB GlaxoSmithKline