PMID

Data

Article Title

Organization

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

Enriching screening libraries with bioactive fragment space.

Beijing University of Technology

Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.

Astrazeneca

Computational Tools To Model Halogen Bonds in Medicinal Chemistry.

Colorado State University

Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.

Kyoto University

Synthesis of novel polybrominated benzimidazole derivatives-potential CK2 inhibitors with anticancer and proapoptotic activity.

Warsaw University of 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

Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.

Christian-Albrechts-University of Kiel

Synthesis of novel chiral TBBt derivatives with hydroxyl moiety. Studies on inhibition of human protein kinase CK2a and cytotoxicity properties.

Warsaw University of Technology

Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.

Siedlce University of Natural Sciences and Humanities

Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.

Astrazeneca

Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.

Astrazeneca

Trimeric hemibastadin congener from the marine sponge Ianthella basta.

Heinrich-Heine University

Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds.

Kyoto University

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

Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.

Cylene Pharmaceuticals

Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

TBA

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.

Millennium Pharmaceuticals

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University of Oxford

Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.

Osi Pharmaceuticals

Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities.

Polaris Pharmaceuticals

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

CK2a and CK2a' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.

The John Paul Ii Catholic University of Lublin

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.

Cylene Pharmaceuticals

Identification of potent ITK inhibitors through focused compound library design including structural information.

Nycomed

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

Ambit Biosciences

Novel 8-arylated purines as inhibitors of glycogen synthase kinase.

Institut Curie

Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid.

Osaka Prefecture University

Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2.

Institute of Biochemistry and Biophysics

Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.

Eberhard-Karls University

Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors.

Istituto Di Ricerche Di Biologia Molecolare &Quot;P. Angeletti

Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water.

Kindai University

Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.

Sichuan University

Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.

Polaris Pharmaceuticals

Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.

Biocon-Bristol Myers Squibb Research and Development Center

The Science and Art of Structure-Based Virtual Screening.

Astrazeneca

Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.

University of North Carolina At Chapel Hill

Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-

Biocon-Bristol Myers Squibb Research and Development Center

Silmitasertib (CX-4945), a Clinically Used CK2-Kinase Inhibitor with Additional Effects on GSK3β and DYRK1A Kinases: A Structural Perspective.

Jagiellonian University

Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.

Al-Azhar University

Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-

Goethe University Frankfurt

Molecular Plasticity of Crystalline CK2α' Leads to KN2, a Bivalent Inhibitor of Protein Kinase CK2 with Extraordinary Selectivity.

Universit£T Zu K£Ln

A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.

University of Cambridge

Recent advances in development of hetero-bivalent kinase inhibitors.

Cha University

Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.

University of North Carolina At Chapel Hill

Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.

Michigan State University

Identification of Thieno[3,2-

Yonsei University College of Medicine

A novel class of selective CK2 inhibitors targeting its open hinge conformation.

University of Trento

Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.

Goethe University Frankfurt

Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α.

University of Cambridge

New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.

Mansoura University

Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity

University of Nottingham

Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Merck

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.

Japan Tobacco

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site.

Saarland University

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action.

University of Lyon

Discovery of 4

TBA

Identification of an indol-based multi-target kinase inhibitor through phenotype screening and target fishing using inverse virtual screening approach.

University of Naples Federico Ii

Small molecule modulators targeting protein kinase CK1 and CK2.

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

Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.

Dana-Farber Cancer Institute

Bioactive metabolites from the endophytic fungus Stemphylium globuliferum isolated from Mentha pulegium.

Heinrich-Heine-Universitat

Cytotoxic metabolites from the fungal endophyte Alternaria sp. and their subsequent detection in its host plant Polygonum senegalense.

Heinrich-Heine-Universit£T

Novel non-ATP competitive small molecules targeting the CK2 α/β interface.

University of Cambridge

Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.

Astrazeneca

Thiazole- and selenazole-comprising high-affinity inhibitors possess bright microsecond-scale photoluminescence in complex with protein kinase CK2.

University of Tartu

Oligo-aspartic acid conjugates with benzo[c][2,6]naphthyridine-8-carboxylic acid scaffold as picomolar inhibitors of CK2.

University of Tartu

Fragment-to-Lead Medicinal Chemistry Publications in 2016.

Astex Pharmaceuticals

A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066.

University of Cambridge

P2X3 andor P2X2/3 receptor antagonist, pharmaceutical composition comprising same, and use thereof

Beijing Tide Pharmaceutical Co.

Spiro compounds as glycosidase inhibitors

Asceneuron

Pyrimidinone derivatives as SHP2 antagonists

Merck Patent

MU opioid receptor modulators

University of California

4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators

Vanderbilt University

Polycyclic pyridone derivative having integrase inhibitory activity

Shionogi

Substituted quinazoline compounds and preparation and uses thereof

Sunshine Lake Pharma

Histone demethylase inhibitors

Celgene Quanticel Research

Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.

University of Texas Southwestern Medical Center

A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases.

The Scripps Research Institute

Azaquinazolinediones chymase inhibitors

Boehringer Ingelheim International

Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.

Hospital Saint-Antoine

2',3'-Dideoxy-N6-cyclohexyladenosine: an adenosine derivative with antagonist properties at adenosine receptors.

Pharmakologisches Institut

Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.

Glaxo Group Research

Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability.

Sandoz Research Institute