141 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.
East China Normal University
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.
Universit£
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
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
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
Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Merck Research Laboratories
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
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.
Merck Research Laboratories
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Bristol-Myers Squibb Research and Development
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Nerviano Medical Sciences
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.
Merck Research Laboratories
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.
University of Nottingham
Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.
Emory University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
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
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.
Teijin Pharma
Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.
TBA
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.
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
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
Abbott Laboratories
Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.
Wyeth Research
C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.
Wyeth Research
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
Harvard Medical School
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
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
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
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.
Serono Pharmaceutical Research Institute
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.
Glaxosmithkline
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
Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.
Merck Research Laboratories
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Merck Research Laboratories
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
Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Merck Research Laboratories
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
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
Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.
The Institute of Cancer Research
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.
Bristol-Myers Squibb
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Novartis Institutes For Biomedical Research
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Novartis Institutes For Biomedical Research
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pfizer
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Merck Research Laboratories
Structure-based lead identification of ATP-competitive MK2 inhibitors.
Merck Research Laboratories
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Merck Research Laboratories
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
5-amino-pyrazoles as potent and selective p38a inhibitors.
Bristol-Myers Squibb Research and Development
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Novartis Institutes For Biomedical Research
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
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
University of Dundee
4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2).
Astrazeneca R & D Lund
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
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Wyeth Research
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.
Wyeth Research
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Amgen
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
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Wyeth Research
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.
Wyeth Research
Guttiferones O and P, prenylated benzophenone MAPKAPK-2 inhibitors from Garcinia solomonensis.
Griffith University
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Novartis Institutes For Biomedical Research
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
C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.
Wyeth Research
Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency.
Pfizer
Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency.
Pfizer
Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.
Johnson & Johnson Pharmaceutical Research & Development
Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Wyeth Research
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Pfizer
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.
Wyeth Research
Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.
Glaxosmithkline
Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.
Wyeth Research
4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.
Wyeth Research
Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.
Bristol Myers Squibb Research and Development
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
Wyeth Research
Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.
Wyeth Research
Phaeochromycins A-E, anti-inflammatory polyketides isolated from the soil actinomycete Streptomyces phaeochromogenes LL-P018.
Wyeth Research
Meroterpenoid MAPKAP (MK2) inhibitors isolated from the indonesian marine sponge Acanthodendrilla sp.
University of British Columbia
Cheilanthane sesterterpenes, protein kinase inhibitors, from a marine sponge of the genus Ircinia.
Astrazeneca R&D Griffith University
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.
Bristol-Myers Squibb Research and Development
Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.
Cardiff University
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Pfizer
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Abbott Laboratories
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.
Glaxosmithkline
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
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Hefei University of Technology
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
Abbott Laboratories
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Abbott Bioresearch Center
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Wyeth Research
New dual inhibitors of EGFR and HER2 protein tyrosine kinases.
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Pfizer
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Bristol-Myers Squibb
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.
Eberhard Karls University T£Bingen
Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.
Boehringer Ingelheim Pharmaceuticals
The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38? MAP kinase inhibitors.
Astrazeneca
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Novartis Institutes For Biomedical Research
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies.
Southeast 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
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.
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.
Abbvie Bioresearch Center
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.
Shanghai Pharmaceuticals Holding
Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.
Novartis Institutes For Biomedical Research
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
Comparison of the structural properties of the active site cavities of human and rat monoamine oxidase A and B in their soluble and membrane-bound forms.
Emory University
Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.
Sibia Neurosciences
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
University of Arizona
Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.
Abbott Laboratories