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208 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28541695 192 Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRa) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs).EBI East China University of Science and Technology
28038328 17 Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3).EBI East China University of Science and Technology
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI Abbvie Bioresearch Center
27750146 58 Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.EBI Chinese Academy of Sciences
28004573 82 Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.EBI The Institute of Cancer Research
28190652 26 Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
27490023 25 Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical 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
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John'S University
27502700 36 Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.EBI Novartis Institutes of Biomedical Research (Nibr)
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
27187609 37 Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight.EBI Novartis Institutes For Biomedical Research
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
27010810 24 Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.EBI Oribase Pharma
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
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
26927423 58 Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.EBI Merck
26897090 18 Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
26698536 56 Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EBI Chinese Academy of Sciences
26774655 32 Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.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
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
25908516 10 Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties.EBI Sichuan University
25835317 63 Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.EBI Sichuan University
25822739 37 Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.EBI Ku Leuven
25474320 10 Nintedanib: from discovery to the clinic.EBI Boehringer Ingelheim Pharma
25036791 56 Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.EBI National Taiwan University
24882675 12 Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
24785465 80 Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.EBI Chinese Academy of Sciences
25462247 20 In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI Fudan University
25409491 83 A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI Zhejiang 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
24456902 14 Synthesis and biological evaluation of novel pazopanib derivatives as antitumor agents.EBI Tianjin University
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
23993328 41 Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.EBI Chinese Academy of Sciences
23838381 38 Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
23937569 22 Selectivity data: assessment, predictions, concordance, and implications.EBI Eli Lilly
23770449 16 Naphthalimides exhibit in vitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs).EBI East China University of Science and Technology
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
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
23628470 40 Discovery of novel 4-(2-fluorophenoxy)quinoline derivatives bearing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
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
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical
23434140 35 Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI East China University of Science and Technology
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
23219325 36 Novel cinnoline-based inhibitors of LRRK2 kinase activity.EBI Elan Pharmaceuticals
23414235 12 Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.EBI Institute of Microbial Chemistry (Bikaken)
23273517 53 Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.EBI National Center For Advancing Translational Sciences
22765894 223 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.EBI Exelixis
23127890 96 SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.EBI Exelixis
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
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
24900421 87 Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.EBI TBA
22980219 55 Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.EBI Takeda Pharmaceutical
22695126 98 Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.EBI Abbott Laboratories
24900482 32 Targeted kinase selectivity from kinase profiling data.EBI TBA
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
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
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
22497760 144 Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.EBI Astrazeneca
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
20570526 84 Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.EBI National Taiwan University
20038108 19 Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.EBI Wyeth Research
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
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute-Bethesda
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
19320489 125 Discovery and development of aurora kinase inhibitors as anticancer agents.EBI Vertex Pharmaceuticals
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
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
12238930 94 Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.EBI Kyowa Hakko Kogyo
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
22056746 53 Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.EBI Boehringer Ingelheim Pharmaceuticals
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
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
21561767 48 Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI Ariad Pharmaceuticals
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
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
21322567 18 Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.EBI University of Strasburg
21316232 41 4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II.EBI Johnson & Johnson Pharmaceutical Research & Development
21273066 83 Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.EBI National University of Ireland
21038853 133 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI Novartis Institutes For Biomedical Research
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
20919678 109 Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI).EBI Boehringer Ingelheim Pharma
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
20817538 16 Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.EBI Novartis Institutes For Biomedical Research
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
18559524 21 BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI Boehringer Ingelheim Austria
16783341 34 Rational design of inhibitors that bind to inactive kinase conformations.EBI Novartis Research Foundation
20472445 23 Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.EBI Ewha Womans University
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
19894727 164 Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.EBI Wyeth Research
20223663 100 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.EBI Wyeth Research
20218619 44 Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen
20188552 75 Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI Wyeth Research
19854649 49 Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI Wyeth Research
19854645 87 Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI Wyeth Research
19646870 34 Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.EBI Ambit Biosciences
20031417 40 Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.EBI Hadassah Hebrew University Hospital
20148563 42 BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.EBI The Institute of Cancer Research
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
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
19364658 113 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Wyeth Research
18723346 26 Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.EBI Amgen
18691885 60 Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.EBI Ariad Pharmaceuticals
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
18602262 56 Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI Glaxosmithkline
18447379 96 Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.EBI Amgen
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI Glaxosmithkline
16570914 32 Identification of potent and selective inhibitors of PDGF receptor autophosphorylation.EBI Kirin Brewery
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
16190746 28 Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.EBI Cnrs Umr-8113
15743179 79 Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.EBI Kirin Brewery
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
12086491 116 Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.EBI Pharmaceutical Research Institute
32832025 20 Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.EBI Jinan University
32292564 138 Efficacy and Tolerability of Pyrazolo[1,5-EBI The Genomics Institute of The Novartis Research Foundation
32292555 44 Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.EBI University of Oxford
31757666 314 Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI Merck
27448775 102 Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase.EBI Shanghai Pharmaceuticals Holding
26844689 22 Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.EBI Chinese Academy of Sciences
30755337 95 Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.EBI Japan Tobacco
31493743 32 Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors.EBI Anadolu University
29522671 80 Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.EBI Chinese Academy of Sciences
31693351 473 Discovery of 4EBI TBA
31250638 34 Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-EBI Chinese Academy of Sciences
31514019 43 Activity of 2,6,9-trisubstituted purines as potent PDGFR? kinase inhibitors with antileukaemic activity.EBI Palack£
31079967 43 Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.EBI School of Marine Science and Technology
30763817 39 Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.EBI University of Naples Federico Ii
30987781 88 Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.EBI Southeast University
31513411 41 Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.EBI Korea University
30508668 62 Discovery of a highly selective FLT3 inhibitor with specific proliferation inhibition against AML cells harboring FLT3-ITD mutation.EBI China Pharmaceutical University
30384048 365 ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI University of Florida
31614258 178 Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.EBI Vichem Chemie Research
26568411 68 Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.EBI Novartis Institutes For Biomedical Research
26505898 123 Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI Novartis Institutes For Biomedical Research
31200237 95 Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.EBI Shanghai Pharmaceuticals Holding
31046271 21 Discovery of ( E)- NEBI Chinese Academy of Sciences
30216852 16 Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety.EBI Jiangxi Science & Technology Normal University
30085668 41 Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.EBI Institute of Cancer Research
30082069 359 ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.EBI Vertex Pharmaceuticals
30078608 44 Discovery of novel Syk/PDGFR-?/c-Kit inhibitors as multi-targeting drugs to treat rheumatoid arthritis.EBI East China University of Science & Technology
29945794 193 ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI Vertex Pharmaceuticals
29544149 5 Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFR? kinase inhibitor for PDGFR? driving chronic eosinophilic leukemia.EBI Chinese Academy of Sciences
29678462 7 Preliminary in vitro and in vivo investigation of a potent platelet derived growth factor receptor (PDGFR) family kinase inhibitor.EBI University of The Pacific
29466002 193 Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.EBI University of Edinburgh
29107542 35 Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.EBI Novartis Institutes For Biomedical Research
29089259 50 Trisubstituted purine inhibitors of PDGFR? and their antileukemic activity in the human eosinophilic cell line EOL-1.EBI Palack£
29107425 90 Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI Korea Institute of Science & Technology (Kist)
28826084 37 Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors.EBI Shenyang Pharmaceutical University
29400470 41 The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.EBI Novartis Institutes For Biomedical Research
28734581 37 Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.EBI Sichuan University and Collaborative Innovation Center
28716639 24 Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
29499108 118 Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.EBI Chinese Academy of Sciences
28956923 34 Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.EBI Chinese Academy of Sciences
28412159 46 Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors.EBI Hangzhou Xixi Hospital
28411455 45 Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization.EBI Shanghai Pharmaceuticals Holding
28714692 232 Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer.EBI University of Chinese Academy of Sciences
21985426 27 Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.BDB Ondokuz Mayis University
27231830 27 Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.BDB Aimst University
15197107 7 Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate.BDB Schering-Plough Research Institute
12616631 18 D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.BDB University of Queensland Brisbane