PMID

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Article Title

Organization

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

Merck

G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.

Universit£

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

Design, synthesis and biological characterization of selective LIMK inhibitors.

Amakem Therapeutics

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

Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.

Vertex Pharmaceuticals

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

In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.

Fudan University

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

Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

Amgen

Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.

TBA

A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.

Nerviano Medical Sciences Oncology

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Nerviano Medical Sciences

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

The selectivity of protein kinase inhibitors: a further update.

University Of Dundee

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

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

Hoffmann-La Roche

Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.

Astrazeneca

Kinase inhibitors: not just for kinases anymore.

Northwestern University

Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.

Millennium Pharmaceuticals

Structure-activity relationship studies of flavopiridol analogues.

Mitotix

2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.

Novartis 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

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277

TBA

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Nerviano Medical Sciences

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

Nerviano Medical Sciences Oncology

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

Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.

University Of Tartu

4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.

Vertex Pharmaceuticals

 

A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation

TBA

 

Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives

TBA

 

Synthesis and protein kinase C inhibitory activities of indane analogs of balanol

TBA

 

Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors

TBA

 

Selective inhibition of the tyrosine kinase pp60^src by analogs of 5,10-dihydropyrimido[4,5-b]quinolin-4(1H)-one

TBA

Carbocyclic 3'-deoxyadenosine-based highly potent bisubstrate-analog inhibitor of basophilic protein kinases.

University Of Tartu

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Abbott Laboratories

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.

Abbott Laboratories

Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases.

Institute Of Organic And Bioorganic Chemistry

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

Chiron

Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.

Boehringer Ingelheim Pharmaceuticals

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.

Università

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Astrazeneca

(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

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Bristol-Myers Squibb

Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.

Eli Lilly

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.

Novartis Pharma

Novel IKK inhibitors: beta-carbolines.

Millennium Pharmaceuticals

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.

Aventis Pharma Deutschland

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? 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

CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.

Shaoxing University

Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.

Vertex Pharmaceuticals

The development of novel and selective p56lck tyrosine kinase inhibitors.

R. W. Johnson Pharmaceutical Research Institute

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

Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.

Eli Lilly

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals

Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.

The Ohio State University

Recent progress towards clinically relevant ATP-competitive Akt inhibitors.

Merck

Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.

Ankara University

Cytotoxic and potent CYP1 inhibitors from the marine algae Cymopolia barbata.

University Of The West Indies

In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.

Abbott Laboratories

Characteristics of 125I-iodocyanopindolol binding to beta-adrenergic and serotonin-1B receptors of rat brain: selectivity of beta-adrenergic agents.

Niigata College Of Pharmacy

 

SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C.

Sphinx Laboratories