PMID

Data

Article Title

Organization

Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c.

Universit£

Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.

Amgen

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 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 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.

Genentech

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

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 and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.

Astex Pharmaceuticals

Structure-based design of low-nanomolar PIM kinase inhibitors.

Biogen Idec

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

Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.

Martin-Luther-University Halle-Wittenberg

Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.

Novartis Institutes For Biomedical Research

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).

Nerviano Medical Sciences

Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.

Merck Research Laboratories

Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.

Genentech

Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.

Pfizer

Synthesis and biological activities of 4-substituted pyrrolo[2,3-a]carbazole Pim kinase inhibitors.

TBA

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

Abbott Laboratories

Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.

Sichuan University

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

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

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

The design, synthesis, and biological evaluation of PIM kinase inhibitors.

Exelixis

Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.

TBA

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

Amgen

Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.

Cylene Pharmaceuticals

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

TBA

Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.

Boehringer Ingelheim Pharmaceuticals

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

The selectivity of protein kinase inhibitors: a further update.

University Of Dundee

Pim2 inhibitors from the Papua New Guinean plant Cupaniopsis macropetala.

Griffith University

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

Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.

Pfizer

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

Novel and selective spiroindoline-based inhibitors of Sky kinase.

Pfizer

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

Ansaris

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

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Novartis Institute For Biomedical Research

The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.

Genzyme

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

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

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

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Nerviano Medical Sciences

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

Abbott Laboratories

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.

Clermont Universit£

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

Glaxosmithkline

A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences

Synthesis, activity evaluation, and docking analysis of barbituric acid aryl hydrazone derivatives as RSK2 inhibitors.

East China University Of Science And Technology

Definition of peptide inhibitors from a synthetic peptide library by targeting gelatinase B/matrix metalloproteinase-9 (MMP-9) and TNF-a converting enzyme (TACE/ADAM-17).

China Pharmaceutical University

Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.

Quaid-I-Azam University

Specialization among iron-sulfur cluster helicases to resolve G-quadruplex DNA structures that threaten genomic stability.

National Institutes Of Health, National Institutes Of Health Biomedical Research Center

Inhibition studies on the membrane-associated phospholipase A2 in vitro and prostaglandin E2 production in vivo of the macrophage-like P388D1 cell. Effects of manoalide, 7,7-dimethyl-5,8-eicosadienoic acid, and p-bromophenacyl bromide.

University Of California San Diego

Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R.

Merck Research Laboratories

Pharmacological characterization of KUR-1246, a selective uterine relaxant.

Kissei Pharmaceutical

Characterization of cloned somatostatin receptors SSTR4 and SSTR5.

University Of Pennsylvania

The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist.

Zeneca Pharmaceuticals

Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity.

Zeneca Pharmaceuticals

Strong solute-solute dispersive interactions in a protein-ligand complex.

University Of Leeds