133 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbvie Bioresearch Center
Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-Binding Pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The University of Tokyo
Synthesis and biological activity of pyrazole analogues of the staurosporine aglycon K252c.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Universit£
Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astex Pharmaceuticals
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Pim kinase inhibitory and antiproliferative activity of a novel series of meridianin C derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Keimyung University
Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Martin-Luther-University Halle-Wittenberg
Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Synthesis and biological activities of 4-substituted pyrrolo[2,3-a]carbazole Pim kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan University
Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The University of Tokyo
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cylene Pharmaceuticals
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Pim2 inhibitors from the Papua New Guinean plant Cupaniopsis macropetala.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Griffith University
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Clermont Universit£
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ludwig-Maximilians University of Munich
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cylene Pharmaceuticals
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes of Biomedical Research
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institute For Biomedical Research
The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genzyme
NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Clermont Université
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nerviano Medical Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Clermont Universit£
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
A small molecule-kinase interaction map for clinical kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
China Pharmaceutical University
Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Spanish National Cancer Research Centre (Cnio)
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of North Carolina At Chapel Hill
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Beijing Normal University
Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi
Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Amgen
Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi
Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Spanish National Cancer Research Centre (Cnio)
Kinase Chemodiversity from the Arctic: The Breitfussins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Uit - The Arctic University of Norway
Targeting the immunity protein kinases for immuno-oncology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
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.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Florida
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbvie Bioresearch Center
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The University of Tokyo
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Pharmaceuticals Holding
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astrazeneca
Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Keimyung University
Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Genentech
Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi Genzyme
Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sanofi Genzyme
Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Dana-Farber Cancer Institute
Synthesis, activity evaluation, and docking analysis of barbituric acid aryl hydrazone derivatives as RSK2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
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).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
China Pharmaceutical University
Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Quaid-I-Azam University
Specialization among iron-sulfur cluster helicases to resolve G-quadruplex DNA structures that threaten genomic stability.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
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.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of California San Diego
Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Merck Research Laboratories
BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Upr 9023
Pharmacological characterization of KUR-1246, a selective uterine relaxant.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Kissei Pharmaceutical
Characterization of cloned somatostatin receptors SSTR4 and SSTR5.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Pennsylvania
The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosine receptor antagonist.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Zeneca Pharmaceuticals
Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Zeneca Pharmaceuticals
Pharmacological characterization of a novel muscarinic partial agonist, YM796, in transfected cells expressing the m1 or m2 muscarinic receptor gene.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Arizona
Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cornell University