102 articles for thisTarget
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Article Title
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Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-Binding Pocket.
The University of Tokyo
Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c.
University of Clermont Auvergne
Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold.
Novartis Institutes For Biomedical Research
Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties.
Mendeleyev University of Chemical Technology
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
Synthesis and activities of new indolopyrrolobenzodiazepine derivatives toward acute myeloid leukemia cells.
University of Clermont Auvergne
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.
Amgen
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.
Amgen
Synthesis of pyrazolo[4,3-a]phenanthridines, a new scaffold for Pim kinase inhibition.
Clermont Universit£
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Pim kinase inhibitory and antiproliferative activity of a novel series of meridianin C derivatives.
Keimyung University
Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Novartis Institutes For Biomedical Research
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.
Merck Research Laboratories
Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
Astrazeneca
Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors.
Clermont Universit£
Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.
Genentech
Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors.
Clermont Universit£
Synthesis and biological activities of 4-substituted pyrrolo[2,3-a]carbazole Pim kinase inhibitors.
TBA
Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.
Cylene Pharmaceuticals
Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound.
The University of Tokyo
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Astrazeneca
Kinase inhibitory potencies and in vitro antiproliferative activities of N-10 substituted pyrrolo[2,3-a]carbazole derivatives.
Clermont Universit£
Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
TBA
Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors.
Clermont Universit£
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.
Spanish National Cancer Research Centre (Cnio)
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
7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
Cylene Pharmaceuticals
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.
Novartis Institutes of Biomedical Research
Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles.
Clermont Université
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
National Human Genome Research Institute
Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.
Clermont Universit£
Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.
Sichuan University
Targeting Death-Associated Protein Kinases for Treatment of Human Diseases: Recent Advances and Future Directions.
Southwest Jiaotong University
β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Novartis Institutes For Biomedical Research
Synthesis of new pyrazolo[4,3-a]phenanthridine Pim-1 inhibitors and evaluation of their cytotoxic activity towards the MOLM-13 acute myeloid leukemia cell line.
University of Clermont Auvergne
Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia.
China Pharmaceutical University
Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors.
Spanish National Cancer Research Centre (Cnio)
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.
Goethe-University Frankfurt
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.
Novartis Institutes For Biomedical Research
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.
University of Oxford
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Amgen
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
Zhejiang University
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
Spanish National Cancer Research Centre (Cnio)
Kinase Chemodiversity from the Arctic: The Breitfussins.
Uit - The Arctic University of Norway
Targeting the immunity protein kinases for immuno-oncology.
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
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Genentech
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
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.
The University of Tokyo
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Astrazeneca
Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors.
Keimyung University
Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.
Genentech
High-content screen using zebrafish (Danio rerio) embryos identifies a novel kinase activator and inhibitor.
West Virginia University
Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.
Sanofi Genzyme
Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II.
Sanofi Genzyme
Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.
University of Oxford
1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
Incyte
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR
Pfizer
Covalent small molecule DCN1 inhibitors and therapeutic methods using the same
The Regents of The University of Michigan
2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof
Shanghai Haiyan Pharmaceutical Technology
(Thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists
Eli Lilly
Diamide compounds having muscarinic receptor antagonist and BETA2 adrenergic receptor agonist activity
Theravance Respiratory
Substituted 1,2,3,4-tetrahydropyrido[3,4-E] pyrrolo[1,2-A]pyrimidines as kinase
Allergan
Studies of the Binding of Modest Modulators of the Human Enzyme, Sirtuin 6, by STD NMR.
University At Albany
Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells.
Shenyang Pharmaceutical University
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.
University of Toronto
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases
Galderma Research & Development
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.
Glaxo Group Research
Cloning, molecular characterization, and chromosomal assignment of a gene encoding a second D1 dopamine receptor subtype: differential expression pattern in rat brain compared with the D1A receptor.
Duke University
Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivo.
Johns Hopkins School of Medicine
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals