70 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
19
Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.
Abbvie Bioresearch Center
6
Imidazopyridine-fused [1,3]-diazepinones part 2: Structure-activity relationships and antiproliferative activity against melanoma cells.
University of Montpellier
18
Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight.
Novartis Institutes For Biomedical Research
27
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.
The University of Tokyo
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
17
Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.
Pfizer
13
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.
Genentech
42
Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.
Genentech
38
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Lexicon Pharmaceuticals
26
Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.
Genentech
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
21
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Pfizer
7
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Ambit Biosciences
2
Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.
The University of Texas At Austin
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
21
Polypharmacological Drug Design Guided by Integrating Phenotypic and Restricted Fragment Docking Strategies.
China Pharmaceutical University
23
Discovery of 5-phenyl-3-ureidothiophene-2-carboxamides as protective agents for ALS patient iPSC-derived motor neurons.
Toray Industries
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
5
Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor.
Westfalian Wilhelms University Muenster (WWU)
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
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
6
Pyrrolidinone Derivatives as NIK Inhibitors for Treating Autoimmune and Inflammatory Diseases.
Smith, Gambrell & Russell
47
Design, Synthesis, and Pharmacological Evaluation of Isoindoline Analogues as New HPK1 Inhibitors.
Shanghai Jiao Tong University
12
Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Novartis
11
Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
Central China Normal University
44
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Hefei University of Technology
36
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.
University of Arkansas For Medical Sciences
46
Discovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology.
University of Arkansas For Medical Sciences
36
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.
University of North Carolina at Chapel Hill
21
Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation.
University of Arkansas For Medical Sciences
42
Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation.
University of Arkansas For Medical Sciences
41
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
9
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia.
University of Regensburg
42
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.
Pfizer
45
Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.
Biogen
25
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
8
Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase.
AstraZeneca
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
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
21
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.
Northwestern University
24
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
15
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
423
PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS
Alexion Pharmaceuticals
7
Inhibiting ataxia telangiectasia and RAD3-related protein (ATR)
Celator Pharmaceuticals
37
Fluorobenzoyl dipeptidyl derivatives as inhibitors of the Fasciola hepatica cysteine protease cathepsin L1.
Dublin City University
2
Dissecting the Multiple Roles of PqsE in Pseudomonas aeruginosa Virulence by Discovery of Small Tool Compounds.
Helmholtz-Institute For Pharmaceutical Research Saarland
8
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Merck Sharpe & Dohme
2
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.
Pharmacia