160 articles for thisTarget
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Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Novartis Institutes For Biomedical Research
Design, synthesis, and biological evaluation of novel 4-anilinoquinazoline derivatives bearing amino acid moiety as potential EGFR kinase inhibitors.
Xuzhou Medical University
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.
Chugai Pharmaceutical
Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives.
University Of Sharjah
Integrated bioinformatics, computational and experimental methods to discover novel Raf/extracellular-signal regulated kinase (ERK) dual inhibitors against breast cancer cells.
Sichuan University
Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.
Hanyang University
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).
Icahn School Of Medicine At Mount Sinai
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.
Univ. Lille
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.
Universit£
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.
Sichuan University
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.
Hanyang University
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Eli Lilly
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.
Astellas Pharma
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.
Sichuan University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.
Hanyang University
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Lexicon Pharmaceuticals
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.
Shenyang Pharmaceutical University
Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.
Development Center For Biotechnology
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.
Peking Union Medical College & Chinese Academy Of Medical Sciences
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Chugai Pharmaceutical
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.
Emory University
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Astrazeneca
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
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.
Sichuan University
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.
Vertex Pharmaceuticals
Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.
RhôNe-Poulenc Rorer
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.
Takeda Pharmaceutical
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
University Of Genoa
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
National Institute Of Biological Sciences
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.
Exelixis
Structure-based optimization of aminopyridines as PKC¿ inhibitors.
Vertex Pharmaceuticals
Design, synthesis and antitumor activities of novel bis-aryl ureas derivatives as Raf kinase inhibitors.
Academy Of Military Medical Sciences
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.
Sichuan University
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Genentech
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.
Ambit Biosciences
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.
Hanyang University
Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
Eberhard Karls University Tuebingen
Dual binding site inhibitors of B-RAF kinase.
Johnson & Johnson Pharmaceutical Research & Development
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Bristol-Myers Squibb Research And Development
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
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.
Osi Pharmaceuticals
Pharmacophore identification of Raf-1 kinase inhibitors.
China Pharmaceutical University
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.
Serono Pharmaceutical Research Institute
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Glaxosmithkline
Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.
Bayer Research Center
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors.
Tsinghua University
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Chugai Pharmaceutical
Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.
Novartis Institutes For Biomedical Research
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.
Millennium Pharmaceuticals
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.
Osi Pharmaceuticals
Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors.
Merck Serono
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Millennium Pharmaceuticals
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Pfizer
Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.
Deciphera Pharmaceuticals
Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line.
Institute Of Science And Technology
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Center For Molecular Medicine Of The Austrian Academy Of Sciences
Rational design of inhibitors that bind to inactive kinase conformations.
Novartis Research Foundation
1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors.
Institute Of Science And Technology
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.
Amgen
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Wyeth Research
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.
The Institute Of Cancer Research
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.
Hanmi Research Center
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.
Boehringer Ingelheim Pharmaceuticals
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
University Of Illinois At Chicago
Virtual screening for Raf-1 kinase inhibitors based on pharmacophore model of substituted ureas.
China Pharmaceutical University
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Glaxosmithkline
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Ariad Pharmaceuticals
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Glaxosmithkline
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.
Wyeth Research
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Boehringer Ingelheim Pharmaceuticals
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
Targegen
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.
Chiron
Rapid computational identification of the targets of protein kinase inhibitors.
University Of Iowa
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.
Astrazeneca
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Novartis Institutes For Biomedical Research
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.
Korea Institute Of Science And Technology
Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent.
Bayer Research Center
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Sichuan University/Collaborative Innovation Center Of Biotherapy
From Lead to Drug Candidate: Optimization of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as Agents for the Treatment of Triple Negative Breast Cancer.
Sichuan University
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.
Chinese Academy Of Sciences
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Genentech
2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAF
Korea Institute Of Science And Technology (Kist)
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
Boehringer Ingelheim Pharmaceuticals
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Merck Research Laboratories
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
Glaxosmithkline
Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold.
National Research Centre (Nrc)
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Research Biomet. Glaxo Wellcome Medicines Research Centre
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
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.
Japan Tobacco
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.
National Research Centre
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.
Indian Institute Of Technology (Bhu)
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors.
China Pharmaceutical University
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.
Merck Research Laboratories
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.
Chung-Ang University
Targeting tropomyosin receptor kinase for cancer therapy.
China Pharmaceutical University
Design, synthesis, and in vitro evaluation of N-(3-(3-alkyl-1H-pyrazol-5-yl) phenyl)-aryl amide for selective RAF inhibition.
Hanyang University
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.
China Pharmaceutical University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
University Of Florida
Discovery of a potent p38?/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.
University Of Sharjah
Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.
Korea Institute Of Science And Technology (Kist)
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.
Shanghai Pharmaceuticals Holding
Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
Chugai Pharmaceutical
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.
University Of Science & Technology (Ust)
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF
Nanjing University
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
Institute Of Cancer Research
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.
Universit£
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
University Of South Australia
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.
Jiangxi Science & Technology Normal University
Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrazolo[3,4-d]pyrimidine derivatives as BRAF
Southern Medical University
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.
China Pharmaceutical University
Pharmacological characterization of (E)-N-(4-fluorobut-2-enyl)-2beta-carbomethoxy-3beta-(4'-tolyl)nortropane (LBT-999) as a highly promising fluorinated ligand for the dopamine transporter.
University Of Tours
Alpha-1 adrenergic receptor binding in aortas from rat and dog: comparison of [3H]prazosin and beta-iodo-[125I]-4-hydroxyphenyl-ethyl-aminomethyl-tetralone.
Unwersity Of Misscuri
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.
Dainippon Sumitomo Pharma
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.
Pfizer
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.
Purdue University