56 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
19
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
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
38
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Lexicon Pharmaceuticals
15
Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.
Boehringer Ingelheim (Canada)
2
Discovery and characterization of novel allosteric FAK inhibitors.
Takeda Pharmaceutical
31
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Exelixis
14
Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Cellzome
37
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Amgen
2
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
37
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
7
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
2
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Center For Molecular Medicine of The Austrian Academy of Sciences
49
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
35
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
28
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
24
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Wyeth Research
27
Discovery of highly potent and selective type I B-Raf kinase inhibitors.
Wyeth Research
24
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.
Wyeth Research
3
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Vertex Pharmaceuticals
40
Structure-Guided Optimization of 2-Aminoquinazoline Hematopoietic Progenitor Kinase 1 Inhibitors for Improved Oral Bioavailability and Synergistic Antitumor Immunity.
China Pharmaceutical University
38
Discovery of 7-(1-methyl-1H-pyrazol-4-yl)-1,6-naphthyridine derivatives as potent inhibitors of rearranged during transfection (RET) and RET solvent-front mutants for overcoming selpercatinib resistance.
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
7
Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1.
Genentech Inc.
13
Discovery of 1(2H)-phthalazinone and 1(2H)-isoquinolinone derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Insilico Medicine Shanghai Ltd
21
Discovery of Pyridine-2-Carboxamides Derivatives as Potent and Selective HPK1 Inhibitors for the Treatment of Cancer.
Insilico Medicine Shanghai Ltd
22
Design, Synthesis, and Biological Evaluation of a Series of Spiro Analogues as Novel HPK1 Inhibitors.
Insilico Medicine Shanghai Ltd
5
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Center for Lymphoid Malignancies
1
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494).
AbbVie Bioresearch Center
5
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Mayo Clinic
25
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Harvard Medical School
3
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Galapagos NV
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
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Eli Lilly
1
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
The Scripps Research Institute
2
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.
University of California Irvine (UCI)
3
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
9
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
AbbVie
47
Design, Synthesis, and Pharmacological Evaluation of Isoindoline Analogues as New HPK1 Inhibitors.
Shanghai Jiao Tong University
21
Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases.
China Pharmaceutical University
11
Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
Central China Normal University
32
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Incyte Research Institute
26
A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics.
University of South Carolina
37
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
25
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
7
Kinase Chemodiversity from the Arctic: The Breitfussins.
Uit - The Arctic University of Norway
2
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
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
34
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.
Sichuan University/Collaborative Innovation Center of Biotherapy
15
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
30
First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
Korea University
4
Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors.
Hokkaido University
15
Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity.
Karo Bio