188 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Design, synthesis, and biological evaluation of novel 4-anilinoquinazoline derivatives bearing amino acid moiety as potential EGFR kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Xuzhou Medical University
Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Design and synthesis of new RAF kinase-inhibiting antiproliferative quinoline derivatives. Part 2: Diarylurea derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Sharjah
Integrated bioinformatics, computational and experimental methods to discover novel Raf/extracellular-signal regulated kinase (ERK) dual inhibitors against breast cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Univ. Lille
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Lexicon Pharmaceuticals
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Development Center For Biotechnology
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Peking Union Medical College & Chinese Academy of Medical Sciences
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Emory University
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Novel triazolopyridylbenzamides as potent and selective p38a inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Genoa
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Institute of Biological Sciences
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Exelixis
Structure-based optimization of aminopyridines as PKC¿ inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Design, synthesis and antitumor activities of novel bis-aryl ureas derivatives as Raf kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eberhard Karls University Tuebingen
Dual binding site inhibitors of B-RAF kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bristol-Myers Squibb Research and Development
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Osi Pharmaceuticals
Pharmacophore identification of Raf-1 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Serono Pharmaceutical Research Institute
Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bayer Research Center
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Tsinghua University
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Millennium Pharmaceuticals
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Osi Pharmaceuticals
Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Serono
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Millennium Pharmaceuticals
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Deciphera Pharmaceuticals
Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Institute of Science and Technology
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Center For Molecular Medicine of The Austrian Academy of Sciences
Rational design of inhibitors that bind to inactive kinase conformations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Research Foundation
1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanmi Research Center
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Illinois At Chicago
Virtual screening for Raf-1 kinase inhibitors based on pharmacophore model of substituted ureas.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ariad Pharmaceuticals
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Targegen
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chiron
High-Throughput Screening Platform in Postnatal Heart Cells and Chemical Probe Toolbox to Assess Cardiomyocyte Proliferation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Christian-Albrechts University of Kiel
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Arkansas For Medical Sciences
Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eternity Bioscience
Therapeutic Potential and Activity Modulation of the Protein Lysine Deacylase Sirtuin 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sapienza University of Rome
Application of Rapidly Accelerating Fibrosarcoma Protein Degraders in Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Usona Institute
Rapid computational identification of the targets of protein kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Iowa
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Design and synthesis of new quinoline derivatives as selective C-RAF kinase inhibitors with potent anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Sharjah
The overview of Mitogen-activated extracellular signal-regulated kinase (MEK)-based dual inhibitor in the treatment of cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhengzhou University
Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Sharjah
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eternity Bioscience
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science and Technology
Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science & Technology (Kist)
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Research Centre (Nrc)
Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Research Biomet. Glaxo Wellcome Medicines Research Centre
Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth-Ayerst Research
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Japan Tobacco
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Research Centre
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Indian Institute of Technology (Bhu)
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chung-Ang University
Targeting tropomyosin receptor kinase for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Hanyang University
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Florida
Discovery of a potent p38?/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Institute of Science & 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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Pharmaceuticals Holding
Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Solution phase parallel synthesis and evaluation of MAPK inhibitory activities of close structural analogues of a Ras pathway modulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Morphochem
Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Science & Technology (Ust)
Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nanjing University
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Institute of Cancer Research
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of South Australia
Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Jiangxi Science & Technology Normal University
Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrazolo[3,4-d]pyrimidine derivatives as BRAF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southern Medical University
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Steady-state kinetic mechanism of Ras farnesyl:protein transferase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Merck Research Laboratories
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.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
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.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Unwersity of Misscuri
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Dainippon Sumitomo Pharma
Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of St. Andrews
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Pfizer
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Purdue University
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Dupont Pharmaceuticals
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sapienza University of Rome