72 articles for thisTarget
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Article Title
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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
Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors.
Institute For Basic Science (Ibs)
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.
Zhengzhou University
Identification of indole-3-carboxylic acids as non-ATP-competitive Polo-like kinase 1 (Plk1) inhibitors.
China Pharmaceutical University
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
University Health Network
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.
Merck Research Laboratories
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
Entremed
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
Entremed
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Elan Pharmaceuticals
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.
Merck Research Laboratories
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.
Janssen Pharmaceutical Companies of Johnson & Johnson
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.
Merck Research Laboratories
4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.
Nerviano Medical Sciences
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Millennium Pharmaceuticals
5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.
Nerviano Medical Sciences
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 imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
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
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.
Glaxosmithkline
Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
Nerviano Medical Sciences
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.
Abbott Laboratories
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors.
Banyu Tsukuba Research Institute
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
Glaxosmithkline
Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects.
Activx Biosciences
Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1.
Shenyang Pharmaceutical University
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.
University of Modena and Reggio Emilia
A comprehensive overview of β-carbolines and its derivatives as anticancer agents.
Xinyang Normal University
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
University of Clermont Auvergne
Structure-activity and mechanistic studies of non-peptidic inhibitors of the PLK1 polo box domain identified through REPLACE.
University of South Carolina
Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential.
West China Hospital
Recent progress in agents targeting polo-like kinases: Promising therapeutic strategies.
Shandong First Medical University & Shandong Academy of Medical Sciences
Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer.
Zentalis Pharmaceuticals
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Discovery of Novel Polo-Like Kinase 1 Polo-Box Domain Inhibitors to Induce Mitotic Arrest in Tumor Cells.
Peking University
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.
Hefei University of Technology
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.
The Institute of Cancer Research
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
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
Vanillin-derived antiproliferative compounds influence Plk1 activity.
Johann-Wolfgang-Goethe University of Frankfurt
Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors.
National Cancer Institute-Frederick
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Merck
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.
Hefei University of Technology
Design, synthesis and biological evaluation of phosphopeptides as Polo-like kinase 1 Polo-box domain inhibitors.
China Pharmaceutical University
Enhancing polo-like kinase 1 selectivity of polo-box domain-binding peptides.
National Cancer Institute-Frederick
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
Ifm Due
Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.
Abbott Laboratories
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.
Weizmann Institute of Science