115 articles for thisTarget
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Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.
Takeda California
Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors.
University of North Carolina at Chapel Hill
Synthesis, biological evaluation, and physicochemical property assessment of 4-substituted 2-phenylaminoquinazolines as Mer tyrosine kinase inhibitors.
Beijing Institute of Pharmacology & Toxicology
Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.
Chinese Academy of Sciences (Cas)
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.
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).
Icahn School of Medicine At Mount Sinai
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute of The Novartis Research Foundation
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.
Shanghai Institute of Materia Medica
Discovery and profiling of a selective and efficacious Syk inhibitor.
Novartis Institutes For Biomedical Research
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.
University of North Carolina at Chapel Hill
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.
Chinese Academy of Sciences
Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.
Eshelman School of Pharmacy�Department of Pharmacology�Lineberger Compreh
Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.
University of North Carolina at Chapel Hill
Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.
Institut Curie
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents.
Beijing Institute of Pharmacology & Toxicology
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Glaxosmithkline
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Amgen
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.
Chinese Academy of Sciences
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
TBA
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
TBA
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Merck Research Laboratories
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Novartis Institute For Biomedical Research
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Center for Lymphoid Malignancies
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Mayo Clinic
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
ARIAD Pharmaceuticals, Inc.
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Galapagos NV
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Tufts Medical Center
A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation.
Pfizer
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.
Bristol-Myers Squibb
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Eli Lilly and Company
The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice.
Astellas Pharma Inc.
Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor.
Pfizer
Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents.
Texas Tech University Health Sciences Center
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.
University of California Irvine (UCI)
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells.
Medical University Innsbruck
CSF1R inhibitors are emerging immunotherapeutic drugs for cancer treatment.
Shenyang Pharmaceutical University
Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies.
Shanghai Institute of Materia Medica
Discovery of Dual MER/AXL Kinase Inhibitors as Bifunctional Small Molecules for Inhibiting Tumor Growth and Enhancing Tumor Immune Microenvironment.
National Health Research Institutes
Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.
Astrazeneca
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Jinan University
Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
Central China Normal University
Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2.
Johann Wolfgang Goethe-University
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Jinan University
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
Massachusetts General Hospital
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.
Jinan University
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6
Sichuan University
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.
University of North Carolina at Chapel Hill
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-
The Genomics Institute of The Novartis Research Foundation
Design and Development of a Chemical Probe for Pseudokinase Ca
Goethe University Frankfurt Am Main
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine derivatives as novel selective Axl inhibitors.
Eisai
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia.
Gwangju Institute of Science and Technology
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
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.
Astrazeneca
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp
Takeda Research In California
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.
University of Michigan
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.
China Pharmaceutical University
Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.
Shenyang Pharmaceutical University
Efficacy and Tolerability of Pyrazolo[1,5-
The Genomics Institute of The Novartis Research Foundation
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors.
Mansoura University
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.
Chinese Academy of Sciences
Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold.
Central China Normal University
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.
Vertex Pharmaceuticals (Europe)
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
Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors.
Korea University
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.
Unc Eshelman School of Pharmacy
Design, synthesis, biological evaluation and cellular imaging of imidazo[4,5-b]pyridine derivatives as potent and selective TAM inhibitors.
Psl Research University
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.
Sichuan University/Collaborative Innovation Center of Biotherapy
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
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.
University of Edinburgh
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.
University of Chinese Academy of Sciences
CRYSTAL OF FUSED TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
Chia Tai Tianqing Pharmaceutical Group
N-((1-BENZYLPIPERIDIN-3-YL)METHYL)-N-(2-METHOXYETHYL)NAPHTHALENE-2-SULFONAMIDE FOR THE TREATMENT OF CANINE COGNITIVE DYSFUNCTION AND OTHER FORMS OF DEMENTIA IN DOGS
Univerza V Ljubljani
[1,2,4]Triazolo derivatives as PDE1 inhibitors for the treatment of diabetes
Eli Lilly
Dipeptidyl ketoamide meta-methoxyphenyl derivatives and uses thereof
Landsteiner Genmed
Tricyclic compounds as glycogen synthase kinase 3 (GSK3) inhibitors and uses thereof
The Broad Institute
Pyrimidine derivative compound, optical isomer thereof, or pharmaceutically acceptable salt thereof, and composition for preventing or treating Tyro 3 related disease comprising same as active ingredient
Korea Research Institute of Chemical Technology
Diazabicyclic substituted imidazopyrimidines and their use for the treatment of breathing disorders
Bayer Aktiengesellschaft
Substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides and methods of making and using same
Mebias Discovery
Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
Boehringer Ingelheim International
Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.
Ondokuz Mayis University
In vitro resistance selections for Plasmodium falciparum dihydroorotate dehydrogenase inhibitors give mutants with multiple point mutations in the drug-binding site and altered growth.
Harvard School of Public Health
Structure-guided design of a high affinity inhibitor to human CtBP.
University of Massachusetts Medical School