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133 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27839918 28 Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).EBI Takeda California, Inc.
27815117 16 Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors.EBI Ocean University of China
27739691 7 Fragment-to-Lead Medicinal Chemistry Publications in 2015.EBI Astex Pharmaceuticals
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's 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
27131066 36 An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Chinese Academy of Sciences
27115835 85 Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.EBI University of Edinburgh
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
27011159 97 Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.EBI Experimental Therapeutics Centre
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
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
27086121 120 Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position.EBI University of Manchester
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
26874741 156 The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.EBI University of Manchester
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
26652860 68 A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.EBI Korea Institute of Science and Technology (KIST)
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
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
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
25625428 10 Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.EBI Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF)
25763473 108 The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.EBI EntreMed Inc.
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24951334 34 Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.EBI Central China Normal University
25589926 20 Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.EBI Astex Pharmaceuticals
25589919 2 RET Kinase Inhibitors May Treat Cancer and Gastrointestinal Disorders.EBI Therachem Research Medilab (India) Pvt. Ltd.
25232968 22 Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation.EBI The University of Arizona
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24904961 27 Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.EBI Qilu Pharmaceutical Co, Ltd
24900886 66 Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.EBI Chinese Academy of Sciences
24779514 128 Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.EBI Gilead Sciences, Inc.
24726806 108 Syk inhibitors with high potency in presence of blood.EBI Novartis Institutes for Biomedical Research
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
24447248 18 Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies.EBI Universit£ di Pisa
24359159 60 Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.EBI AstraZeneca
24183742 40 Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.EBI Chinese Academy of Sciences
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.
23993328 41 Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.EBI Chinese Academy of Sciences
23999040 27 Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.EBI Nanjing University of Technology
23768909 50 Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.EBI Novartis Institutes for BioMedical Research
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
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, Inc.
23474386 26 Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.EBI Chinese Academy of Sciences
23498918 41 Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.EBI Takeda Pharmaceutical Company Limited
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
22521646 38 Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.EBI Rhône-Poulenc Rorer
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 Ltd
23098265 46 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.EBI University of Genoa
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 Research and Development
22257213 98 Discovery and development of spleen tyrosine kinase (SYK) inhibitors.EBI Rigel, Inc.
22863529 31 Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.EBI Chinese Academy of Sciences
22559926 6 Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors.EBI University of Gothenburg
22394077 19 Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.EBI Hoffmann-La Roche Inc.
22452518 22 Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.EBI Sichuan University
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
22465635 95 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI Abbott Laboratories
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.
21608528 166 Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.EBI Merck Research Laboratories
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
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
20117004 68 Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.EBI University of Milano-Bicocca
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
19320489 125 Discovery and development of aurora kinase inhibitors as anticancer agents.EBI Vertex Pharmaceuticals (Europe) Ltd.
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
17113292 73 Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.EBI TargeGen, Inc.
22136433 67 7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.EBI Ludwig-Maximilians University of Munich
22154349 123 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences srl
22056746 53 Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.EBI Boehringer-Ingelheim Pharmaceuticals, Inc.
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
22018461 41 Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).EBI Bristol-Myers Squibb Research and Development
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
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
21724393 74 Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors.EBI National Tsing Hua University
21561767 48 Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI ARIAD Pharmaceuticals, Inc.
21517068 45 Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.EBI East China University of Science and Technology
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
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
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.
21341678 49 Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.EBI Millennium Pharmaceuticals, Inc.
21316232 41 4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II.EBI Johnson& Johnson Pharmaceutical Research& Development LLC
20961062 42 Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.EBI Pfizer Inc.
20925433 21 Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.EBI Aristotle University of Thessaloniki
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
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20409618 31 Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.EBI Technische Universit£t Braunschweig
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
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
19646870 34 Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.EBI Ambit Biosciences Inc.
20148563 42 BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.EBI Institute of Cancer Research
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
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences Srl
19754199 29 Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.EBI Ambit Biosciences
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
19053769 8 Synthesis, modeling, and RET protein kinase inhibitory activity of 3- and 4-substituted beta-carbolin-1-ones.EBI Universita di Milano
18313174 26 Synthesis and biological evaluation of diversely substituted indolin-2-ones.EBI Université Blaise Pascal
17185414 30 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI Genomics Institute of the Novartis Research Foundation
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.
17499504 5 Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones.EBI Università di Milano
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
16610779 10 Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.EBI Università di Padova
17884497 14 The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.BDB GlaxoSmithKline
16951187 11 AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.BDB Amgen