192 articles for thisTarget
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Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet?-cells from apoptosis.
East China Normal University
Discovery of new Syk inhibitors through structure-based virtual screening.
Second Military Medical University
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).
Takeda California
Identification of 4-(2-furanyl)pyrimidin-2-amines as Janus kinase 2 inhibitors.
Central China Normal University
Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.
Merck
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.
Southeast University
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.
Nerviano Medical Sciences
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
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
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
Kangwon National University
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.
Sichuan University
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Novartis Institutes For Biomedical Research
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.
Hanyang 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.
Nerviano Medical Sciences
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.
Astellas Pharma
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Genomics Institute Of The Novartis Research Foundation
Discovery and profiling of a selective and efficacious Syk inhibitor.
Novartis Institutes For Biomedical Research
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Merck
LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors.
Sichuan University
Application of cultured human mast cells (CHMC) for the design and structure-activity relationship of IgE-mediated mast cell activation inhibitors.
Amarit Bioscience
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Vertex Pharmaceuticals
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Lexicon Pharmaceuticals
Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.
Nimbus Discovery
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Galapagos
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Gilead Sciences
Syk inhibitors with high potency in presence of blood.
Novartis Institutes For Biomedical Research
Phenyl carboxamide analogues as spleen tyrosine kinase (syk) inhibitors.
Dart Neuroscience
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.
Hoffmann-La Roche
Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.
University Of Zurich
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.
Zhejiang University
Discovery of ZAP70 inhibitors by high-throughput docking into a conformation of its kinase domain generated by molecular dynamics.
University Of Zurich
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Califia Bio
Inhibitors of switch kinase 'spleen tyrosine kinase' in inflammation and immune-mediated disorders: a review.
Punjabi University
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase
Genomics Institute Of The Novartis Research Foundation
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
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Glaxosmithkline
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.
Cellzome
Rational design of highly selective spleen tyrosine kinase inhibitors.
Hoffmann-La Roche
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Abbott Laboratories
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
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
Hanmi Research Center
X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.
Sanofi Us
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.
Vertex Pharmaceuticals
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.
Boehringer Ingelheim Pharmaceuticals
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.
Glaxosmithkline
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
National Cancer Institute-Bethesda
Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.
Kissei Pharmaceutical
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
A photoswitchable ITAM peptidomimetic: synthesis and real time surface plasmon resonance (SPR) analysis of the effects of cis-trans isomerization on binding.
Utrecht University
Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.
Kissei Pharmaceutical
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.
Kissei Pharmaceutical
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
Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand.
Utrecht University
Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.
Kyoto 619-0216
Potent small molecule inhibitors of spleen tyrosine kinase (Syk).
Aventis Pharmaceuticals
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Glaxosmithkline
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Glaxosmithkline
7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Ludwig-Maximilians University Of Munich
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Genentech
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
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
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.
Bristol-Myers Squibb
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pfizer
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Nerviano Medical Sciences
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Glaxosmithkline
5-amino-pyrazoles as potent and selective p38a inhibitors.
Bristol-Myers Squibb Research And Development
Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.
Nerviano Medical Sciences
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
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
Genentech
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Cgi Pharmaceuticals
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.
Johnson & Johnson Pharmaceutical Research & Development
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.
Vertex Pharmaceuticals
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Glaxosmithkline
Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors.
Sichuan University
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).
Vertex Pharmaceuticals
Identification of novel protein kinase CK1 delta (CK1delta) inhibitors through structure-based virtual screening.
Università
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Tanabe Research Laboratories Usa
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
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.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Abbott Bioresearch Center
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Bristol-Myers Squibb
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.
Kyoto 619-0216
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.
Boehringer Ingelheim Pharmaceuticals
Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).
Boehringer Ingelheim Pharmaceuticals
Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.
Boehringer Ingelheim Pharmaceuticals
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
Boehringer Ingelheim Pharmaceuticals
Design and synthesis of non-peptidic inhibitors for the Syk C-terminal SH2 domain based on structure-based in-silico screening.
Waseda University
Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization.
Purdue University
1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
Novartis Institutes For Biomedical Research
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abbvie Bioresearch Center
Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease.
Glaxosmithkline R&D
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
Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.
Carna Biosciences
Drug-target interactions that involve the replacement or displacement of magnesium ions.
Bristol-Myers Squibb Research And Development
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
Shaanxi University Of Science & Technology
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.
Korea Institute Of Science And Technology (Kist)
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.
The Ohio State University
Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents.
Solapur University
Kinetic characterization of a slow-binding inhibitor of Bla2: thiomaltol.
Baylor University
Acetaldehyde-derived modifications on cytosolic human carbonic anhydrases.
University Of Tampere And Tampere University Hospital
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.
University Of Manchester
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.
Eli Lilly
Development of new and selective Trypanosoma cruzi trans-sialidase inhibitors from sulfonamide chalcones and their derivatives.
University Of British Columbia
Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors.
University Of California San Diego
[125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.
Nida Addiction Research Center
Synthesis and molecular modelling of novel substituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase-A inhibitors.
UniversitÀ
Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.
Smithkline Beecham Pharmaceuticals
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.
Acadia Pharmaceuticals
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.
Gsk
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
Glaxosmithkline
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Merck Research Laboratories
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Abbott Laboratories
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
National Health Research Institutes
Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.
Hebrew University Of Jerusalem
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.
University Of Auckland