101 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Data
Article Title
Organization
52
First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-¿B Activity As Novel Anticancer Agents.
Saarland University
25
Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors.
Novartis Institutes For Biomedical Research
22
Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.
Experimental Therapeutics Centre
23
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Novartis Institutes For Biomedical Research
6
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
16
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.
University of South Australia
61
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
14
Discovery of 4-(dihydropyridinon-3-yl)amino-5-methylthieno[2,3-d]pyrimidine derivatives as potent Mnk inhibitors: synthesis, structure-activity relationship analysis and biological evaluation.
University of South Australia
28
Inhibitors of c-Jun N-terminal kinases: an update.
Eberhard Karls Universit£T T£Bingen
39
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Nerviano Medical Sciences
7
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Astex Pharmaceuticals
37
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.
Nerviano Medical Sciences
26
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase
Genomics Institute of The Novartis Research Foundation
31
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
1
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
16
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.
TBA
37
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
36
1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
RhôNe-Poulenc Rorer
8
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
18
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
29
Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.
Spanish National Cancer Research Centre (Cnio)
7
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
50
Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Nerviano Medical Sciences
15
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
43
Design, Synthesis, and Evaluation of Novel ROCK Inhibitors for Glaucoma Treatment: Insights into In Vitro and In Vivo Efficacy and Safety.
Shandong First Medical University & Shandong Academy of Medical Sciences
28
Discovery of Novel SIK2/3 Inhibitors for the Potential Treatment of MEF2C+ Acute Myeloid Leukemia (AML).
Insilico Medicine Shanghai Ltd.
25
Discovery of Potent and Selective MNK Kinase Inhibitors for the Treatment of Leukemia.
Northwestern University
50
Development of a Second-Generation, In Vivo Chemical Probe for PIKfyve.
University of North Carolina at Chapel Hill
5
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Center for Lymphoid Malignancies
7
Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.
Nerviano Medical Sciences
3
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Galapagos NV
3
NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.
Nerviano Medical Sciences Srl
8
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Tufts Medical Center
1
A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation.
Pfizer
1
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Eli Lilly
28
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.
Bayer AG
3
A Potent and Selective ULK1 Inhibitor Suppresses Autophagy and Sensitizes Cancer Cells to Nutrient Stress.
Michigan State University
61
Discovery and Characterization of Selective, First-in-Class Inhibitors of Citron Kinase.
Lerner Research Institute
5
Discovery of D25, a Potent and Selective MNK Inhibitor for Sepsis-Associated Acute Spleen Injury.
Shandong First Medical University
15
MNK, mTOR or eIF4E-selecting the best anti-tumor target for blocking translation initiation.
Shandong University
45
Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma.
China Pharmaceutical University
27
Design, synthesis and biological evaluation of 4-(indolin-1-yl)-6-substituted-pyrido[3,2-d]pyrimidine derivatives as Mnk1/2 inhibitors.
Shenyang Pharmaceutical University
48
Medicinal chemistry approaches to target the MNK-eIF4E axis in cancer.
Northwestern University
30
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
Galapagos
29
Small-Molecule Fms-like Tyrosine Kinase 3 Inhibitors: An Attractive and Efficient Method for the Treatment of Acute Myeloid Leukemia.
Nanjing University of Chinese Medicine
37
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
12
Using Imidazo[2,1-
Ocean University of China and Laboratory For Marine Drugs and Bioproducts
4
Overcoming Paradoxical Kinase Priming by a Novel MNK1 Inhibitor.
Universitat Ramon Llull
56
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Bristol Myers Squibb
6
Recent development of BTK-based dual inhibitors in the treatment of cancers.
Nantong University
36
Fragment-to-Lead Medicinal Chemistry Publications in 2020.
Vrije Universiteit Amsterdam
20
A small molecule-kinase interaction map for clinical kinase inhibitors.
Ambit Biosciences
12
Progress in developing MNK inhibitors.
Ocean University of China and Laboratory For Marine Drugs and Bioproducts
24
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
University of North Carolina at Chapel Hill
60
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Bristol Myers Squibb
17
Design, synthesis and biological evaluation of imidazopyridazine derivatives containing isoquinoline group as potent MNK1/2 inhibitors.
China Pharmaceutical University
66
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.
University of Sussex
29
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Sichuan University/Collaborative Innovation Center of Biotherapy
28
Discovery of indazole-pyridinone derivatives as a novel class of potent and selective MNK1/2 kinase inhibitors that protecting against endotoxin-induced septic shock.
Ryvu Therapeutics
41
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
9
Biological Evaluation of Selected Flavonoids as Inhibitors of MNKs Targeting Acute Myeloid Leukemia.
The Chinese University of Hong Kong (Shenzhen)
29
Design, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors.
China Pharmaceutical University
56
Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2.
A*Star
6
Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.
University of South Australia
28
Targeting the immunity protein kinases for immuno-oncology.
China Pharmaceutical University
9
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
2
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
8
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.
Novartis Institutes For Biomedical Research
16
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
55
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
7
Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design.
Shenyang Pharmaceutical University
26
Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia.
A*Star
34
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.
Korea Institute of Science & Technology (Kist)
24
Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia.
University of South Australia
26
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition.
Effector Therapeutics
2
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.
Chinese Academy of Sciences
31
MACROCYCLIC BRANCHED 3-FLUORO-BUT-3-ENAMIDES AS INHIBITORS OF MCL-1
Janssen Pharmaceutica
13
Disubstituted compounds for treatment of medical disorders
Achillion Pharmaceuticals
5
Oxazoline pseudodimers, pharmaceutical compositions and the use thereof
Purdue Pharma
220
Substituted benzamides and substituted pyridinecarboxamides as Btk inhibitors
Merck Sharp & Dohme
6
Biotransformation of dehydroepiandrosterone with Macrophomina phaseolina and ß-glucuronidase inhibitory activity of transformed products.
University of Karachi
15
2-Heteroarylidene-1-indanone derivatives as inhibitors of monoamine oxidase.
North-West University
24
Amide or urea containing benzothiazole inhibitors of endothelial lipase
Bristol Myers Squibb
20
Method for the treatment of neurological disorders by enhancing the activity of beta-glucocerebrosidase
Amicus Therapeutics
21
Monoamine oxidase inhibitory activity of 2-aryl-4H-chromen-4-ones.
Birla Institute of Technology
5
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.
Universit&Aagrove
5
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.
Bayer
9
Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.
Ariad Pharmaceuticals
17
Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1).
Duquesne University