PMID

Data

Article Title

Organization

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.

Merck

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

Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.

Central University

Evaluation of Improved Glycogen Synthase Kinase-3a Inhibitors in Models of Acute Myeloid Leukemia.

Technische Universit£T Darmstadt

Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.

University Of Cambridge

Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.

Eli Lilly

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.

The Institute Of Cancer Research

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

Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.

Technische Universit£T Darmstadt

The design and synthesis of potent and selective inhibitors of Trypanosoma brucei glycogen synthase kinase 3 for the treatment of human african trypanosomiasis.

University Of Dundee

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.

Universitat De Barcelona

3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3-b]pyridine-5-carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3.

Technische Universit£T Braunschweig

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

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.

Cellzome

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.

Cnrs

Identification of pyrimidine derivatives as hSMG-1 inhibitors.

Pfizer

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Abbott Laboratories

Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.

Technische Universit£T Darmstadt

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Abbott Laboratories

Pharmacological inhibitors of glycogen synthase kinase 3.

The Rockefeller University

Discovery of potent and bioavailable GSK-3beta inhibitors.

Roche Palo Alto

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Kinetic studies and bioactivity of potential manzamine prodrugs.

The University Of Mississippi

2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).

Kemia

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

Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.

Glaxosmithkline

Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.

Celgene

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.

Technische Universit£T Darmstadt

Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.

National University Of Ireland

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.

Cyclacel

Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.

Universit£

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

Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

Wyeth Research

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.

Université

Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.

Roche Research Center

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 of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.

Chiron

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Johnson & Johnson Pharmaceutical Research And Development

Designing modulators of dimethylarginine dimethylaminohydrolase (DDAH): a focus on selectivity over arginase.

Christian-Albrechts-University

Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors.

Shandong University

Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.

University Of Alexandria

Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.

Wyeth Research

Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.

Abbott Laboratories

Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.

Sapienza University Of Rome

2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships.

Neuroscience

2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 1. Structure-Activity Relationships and Optimization of Heterocyclic Substituents.

Neuroscience

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.

University Of Arizona Tucson