82 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
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
Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ocean University of China
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China University of Science & Technology
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Southeast University
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Green Valley Research Institute
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
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
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Korea Research Institute of Chemical Technology
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
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
Design and Synthesis of Potent Bivalent Peptide Agonists Targeting the EphA2 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
State University of New York
Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Exelixis
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cellzome
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
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
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ansaris
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
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ariad Pharmaceuticals
Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
East China University of Science and Technology
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Millennium Pharmaceuticals
The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ansaris
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
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cgi Pharmaceuticals
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chugai Pharmaceutical
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Zurich
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
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
c-Src protein kinase inhibitors block assembly and maturation of dengue virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Harvard Medical School
Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
A small molecule-kinase interaction map for clinical kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bicycletx
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Pharmaceuticals Holding
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
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-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbvie Bioresearch Center
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Chinese Academy of Sciences
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University/Collaborative Innovation Center of Biotherapy
Reduction of Circulating Cancer Cells and Metastases in Breast-Cancer Models by a Potent EphA2-Agonistic Peptide-Drug Conjugate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of California
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Jinan University
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Pharmaceuticals Holding
One-Bead-Two-Compound Thioether Bridged Macrocyclic?-AApeptide Screening Library against EphA2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of South Florida
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Chinese Academy of Sciences