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245 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
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
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI
Chinese Academy Of Sciences
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI
Southeast University
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).EBI
Chinese Academy Of Sciences
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
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
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).EBI
Green Valley Research Institute
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors.EBI
Jiangxi Science And Technology Normal University
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety.EBI
Jiangxi Science And Technology Normal University
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EBI
Chinese Academy Of Sciences
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
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.EBI
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.EBI
Univ. Lille
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.EBI
Universit£
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI
Sichuan University
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
Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.EBI
Christian-Albrechts-University Of Kiel
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.EBI
Genomics Institute Of The Novartis Research Foundation
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.EBI
Ku Leuven
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.EBI
Chinese Academy Of Sciences
Nintedanib: from discovery to the clinic.EBI
Boehringer Ingelheim Pharma
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.EBI
Duquesne University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.EBI
Shenyang Pharmaceutical University
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
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI
Nerviano Medical Sciences
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
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.EBI
Shenyang Pharmaceutical University
Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.EBI
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI
Zhejiang University
Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.EBI
Southeast University
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.EBI
Novartis Institutes For Biomedical Research
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.EBI
Duquesne University
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents.EBI
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.EBI
Qilu Pharmaceutical
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.EBI
Chinese Academy Of Sciences
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.EBI
Development Center For Biotechnology
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
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI
Nerviano Medical Sciences
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.EBI
Chinese Academy Of Sciences
Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.EBI
Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University)
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
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.EBI
Roche Palo Alto
Quinazoline-based multi-tyrosine kinase inhibitors: synthesis, modeling, antitumor and antiangiogenic properties.EBI
University Of Padova
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
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
Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.EBI
Pfizer
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
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI
Takeda Pharmaceutical
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
Synthesis and biological activity of 5-chloro-N4-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.EBI
Duquesne University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI
Exelixis
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents.EBI
Duquesne University
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
Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI
Heinrich-Heine University
Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.EBI
Institute Of Microbial Chemistry (Bikaken)
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.EBI
National Center For Advancing Translational Sciences
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.EBI
Exelixis
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.EBI
Exelixis
Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.EBI
Takeda Pharmaceutical
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
Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.EBI
TBA
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.EBI
University Of Genoa
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI
National Institute Of Biological Sciences
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI
Exelixis
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
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.EBI
Janssen Pharmaceutical Companies Of Johnson & Johnson
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.EBI
Duquesne University
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
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
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
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
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.EBI
Astrazeneca
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI
Abbott Laboratories
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.EBI
TBA
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.EBI
Duquesne University
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.EBI
Chinese Academy Of Sciences
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
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.EBI
Duquesne University
A quantitative analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
Discovery and development of aurora kinase inhibitors as anticancer agents.EBI
Vertex Pharmaceuticals
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI
Harvard Medical School
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
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.EBI
Amgen
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI
University Of Oxford
Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI
Osi Pharmaceuticals
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.EBI
Johnson & Johnson Pharmaceutical Research & Development
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
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
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.EBI
Hoffmann-La Roche
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
Designed multiple ligands. An emerging drug discovery paradigm.EBI
Organon Laboratories
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.EBI
Novartis Pharma
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
Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI
Millennium Pharmaceuticals
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
N¿?¿-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.EBI
Duquesne University
VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.EBI
University Of Kentucky
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI
Glaxosmithkline
Effects of the indolocarbazole 3744W on the tyrosine kinase activity of the cytoplasmic domain of the platelet-derived growth factor beta-receptor.EBI
Wellcome Research Laboratories
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).EBI
Millennium Pharmaceuticals
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.EBI
Astrazeneca
Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.EBI
Shenyang Pharmaceutical University
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.EBI
Shionogi
N¿?¿-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.EBI
Duquesne University
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
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
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI
RhôNe-Poulenc Rorer
Comprehensive analysis of kinase inhibitor selectivity.EBI
Ambit Biosciences
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
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
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI
Ariad Pharmaceuticals
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
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.EBI
TBA
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
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
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
Identification of potent ITK inhibitors through focused compound library design including structural information.EBI
Nycomed
Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.EBI
Shanghai Hengrui Pharmaceuticals
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
Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.EBI
Astrazeneca
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.EBI
Industrial Technology Research Institute
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
Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.EBI
Novartis Institutes For Biomedical Research
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI
Ambit Biosciences
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI
Boehringer Ingelheim Austria
Rational design of inhibitors that bind to inactive kinase conformations.EBI
Novartis Research Foundation
Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish.EBI
Dana-Farber Cancer Institute
Discovery of pyrrole-indoline-2-ones as Aurora kinase inhibitors with a different inhibition profile.EBI
Development Center For Biotechnology
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.EBI
Duquesne University
The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.EBI
Duquesne University
Selectively nonselective kinase inhibition: striking the right balance.EBI
Schering-Plough
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI
Cgi Pharmaceuticals
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.EBI
Ambit Biosciences
Labeled 3-aryl-4-indolylmaleimide derivatives and their potential as angiogenic PET biomarkers.EBI
Hadassah Hebrew University Hospital
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.EBI
The Institute Of Cancer Research
Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.EBI
4Sc
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
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
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
 
The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-
TBA
 
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylationEBI
TBA
 
Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivativesEBI
TBA
 
Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitorsEBI
TBA
Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.EBI
University Of Regensburg
N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.EBI
4Sc
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.EBI
Novartis Institutes For Biomedical Research
5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.EBI
Mahidol University
Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.EBI
Astrazeneca R&D Boston
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
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI
Glaxosmithkline
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.EBI
Amgen
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
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.EBI
Duquesne University
Structure and regulation of the human Nek2 centrosomal kinase.EBI
University Of Oxford
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI
Genomics Institute Of The Novartis Research Foundation
Entry into a new class of protein kinase inhibitors by pseudo ring design.EBI
Novartis Institutes For Biomedical Research
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI
Glaxosmithkline
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI
Abbott Laboratories
4-Amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes as potent FLT-3 inhibitors.EBI
Johnson And Johnson Pharmaceutical Research And Development
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
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
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
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.EBI
Targegen
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.EBI
University Of Auckland
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
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.EBI
Abbott Laboratories
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.EBI
University Of Regensburg
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.EBI
Pharmaceutical Research Institute
(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
Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.EBI
Korea Research Institute Of Chemical Technology
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
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.EBI
Johnson & Johnson Pharmaceutical Research And Development
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
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
A small molecule-kinase interaction map for clinical kinase inhibitors.EBI
Ambit Biosciences
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
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.EBI
In Vivo Sciences Millennium Pharmaceuticals
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.EBI
Kirin Brewery
Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.EBI
Sugen
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
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.EBI
Pharmaceutical Research Institute
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
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.EBI
Aventis Pharmaceuticals
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI
Johnson & Johnson Pharmaceutical Research & Development
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.EBI
Kyowa Hakko Kogyo
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
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI
Abbott Bioresearch Center
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI
Merck Research Laboratories
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.EBI
Novartis
Design and synthesis of a pyridone-based phosphotyrosine mimetic.EBI
Cadus Pharmaceutical
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
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
A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives.EBI
RhôNe-Poulenc Rorer
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.BDB
King Fahd University Of Petroleum & Minerals
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.BDB
Shandong University
Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.BDB
Glaxosmithkline
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies.BDB
Aimst University
Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.BDB
Neurocrine Biosciences
Identification and characterization of a novel RF-amide peptide ligand for orphan G-protein-coupled receptor SP9155.BDB
Schering-Plough Research Institute
ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB
Abbott Laboratories
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.BDB
UniversitÉ
The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition.BDB
University Of California San Francisco
Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors.BDB
Gsk
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.BDB
Abbott Laboratories
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.BDB
Gsk
Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.BDB
Genentech
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent.BDB
Johnson & Johnson Pharmaceutical
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.BDB
Vernalis (R&D
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.BDB
Plexxikon
A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity.BDB
Duke University Medical Center
Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity.BDB
German Cancer Research Center
A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.BDB
Axys Pharmaceuticals
Structure-Based Design of Novel HIV-1 Protease Inhibitors To Combat Drug Resistance.BDB
Purdue University
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.BDB
Incyte
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.BDB
Abbott Laboratories
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.BDB
University Of Michigan
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.BDB
Abbott Laboratories
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.BDB
University Of Antwerp
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.BDB
Merck Research Laboratories
Selectively guanidinylated derivatives of neamine. Syntheses and inhibition of anthrax lethal factor protease.BDB
Hawaii Biotech
Discovery of a series of hydroximic acid derivatives as potent histone deacetylase inhibitors.BDB
Qingdao University
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.BDB
Universita Di Siena
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.BDB
Linkoping University