187 articles for thisTarget
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Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.
Takeda Pharmaceutical
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.
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
Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.
Merck Research Laboratories
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
Merck Research Laboratories
Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.
Merck Research Laboratories
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.
Astrazeneca
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.
Astellas Pharma
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.
Merck
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.
Merck Research Laboratories
Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4.
Merck Research Laboratories
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Vertex Pharmaceuticals
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 of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
Lexicon Pharmaceuticals
Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.
Nimbus Discovery
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Bristol-Myers Squibb Research and Development
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Glaxosmithkline
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
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.
Merck Research Laboratories
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
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.
Sichuan University
Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.
Janssen Pharmaceutical Companies of Johnson & Johnson
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.
Abbott Laboratories
Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.
Amri
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.
TBA
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
TBA
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.
Merck Research Laboratories
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.
Vertex Pharmaceuticals
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
National Cancer Institute-Bethesda
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
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
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Ansaris
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
Vertex Pharmaceuticals
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
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Center For Molecular Medicine of The Austrian Academy of Sciences
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.
Vertex Pharmaceuticals
IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding.
Ucb Pharma
Novel IRAK4 Inhibitors for Treating Asthma, COPD, Cancer, Autoinflammatory Diseases, and Autoimmune Diseases.
Smith, Gambrell & Russell
Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.
Zhejiang University
Design, synthesis and pharmacological evaluation of 2,3-dihydrobenzofuran IRAK4 inhibitors for the treatment of diffuse large B-cell lymphoma.
China Pharmaceutical University
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Biocon-Bristol Myers Squibb Research and Development Center
In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
Pfizer
Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
Central China Normal University
An overview on the recent developments of 1,2,4-triazine derivatives as anticancer compounds.
Universita Degli Studi Di Palermo
Design, synthesis, and pharmacological evaluation of N-(3-carbamoyl-1H-pyrazol-4-yl)-1,3-oxazole-4-carboxamide derivatives as interleukin-1 receptor-associated kinase 4 inhibitors with reduced potential for cytochrome P450 1A2 induction.
Astellas Pharma
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Bristol-Myers Squibb Research & Development
Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
Novartis Institutes For Biomedical Research
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-
Biocon-Bristol Myers Squibb Research and Development Center
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Astrazeneca
Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
Amgen
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.
China Pharmaceutical University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Hefei University of Technology
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
Abbott Bioresearch Center
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.
Astrazeneca
Novel Tricyclic Heteroaryl Compounds as IRAK4 Inhibitors for Treating Cancer, Autoimmune and Inflammatory Diseases.
Smith, Gambrell & Russell
Discovery of 5-Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors.
Rigel Pharmaceuticals
Discovery of Highly Potent and Selective IRAK1 Degraders to Probe Scaffolding Functions of IRAK1 in ABC DLBCL.
Janssen Research & Development
Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma.
China Pharmaceutical University
Thienopyridinyl and Thiazolopyridinyl Compounds as IRAK4 Inhibitors.
Smith, Gambrell & Russell
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.
Dana-Farber Cancer Institute
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.
Astrazeneca
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.
Chinese Academy of Sciences
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1.
Bristol Myers Squibb
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors.
Vertex Pharmaceuticals
Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors.
Zhejiang Hisun Pharmaceutical
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies.
Aurigene Discovery Technologies
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.
Biocon Bristol Myers Squibb Research Center
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.
Merck Research Laboratories
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.
Genentech
Targeting the immunity protein kinases for immuno-oncology.
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.
University of Florida
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88
Astrazeneca
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.
Takeda Pharmaceutical
PROTAC Degradation of IRAK4 for the Treatment of Neurodegenerative and Cardiovascular Diseases.
Usona Institute
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Dana-Farber Cancer Institute
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 potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4.
Amgen
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Astrazeneca
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
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Merck
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.
Korea Institute of Science & Technology (Kist)
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.
Bristol-Myers Squibb
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88
Astrazeneca
Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.
Astrazeneca
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Pfizer
Substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said substituted indazoles, and use of said substituted indazoles to produce drugs
Bayer Pharma Aktiengesellschaft
Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases
Bayer Pharma Aktiengesellschaft
SULFOXIMIDE SUBSTITUTED INDAZOLE IRAK4 KINASE INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF
Shanghai Xunhe Pharmaceutical Technology Co.
Pyrazole compounds, pharmaceutical compositions thereof and use thereof
Artivila (Shenzhen) Innovation Center
IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS IRAK4 INHIBITORS AND THEIR USE IN THE TREATMENT OF DISEASE
Biogen Ma
MULTI-CYCLIC IRAK AND FLT3 INHIBITING COMPOUNDS AND USES THEREOF
Children'S Hospital Medical Center
Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
Children'S Hospital Medical Center
Isothiazolo[5,4-D]pyrimidine compound as IRAK4 inhibitor
Chia Tai Tianqing Pharmaceutical Group
Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
Arvinas Operations
Substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said new substituted indazoles, and use of said new substituted indazoles to produce drugs
Bayer Pharma Aktiengesellschaft
Indazole amine derivative, preparation method therefor and medical use thereof
Zhejiang Hisun Pharmaceutical
Heteroaryl substituted pyridyl compounds useful as kinase modulators
Bristol-Myers Squibb
2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs
Bayer Pharma Aktiegesellschaft
Substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said new substituted indazoles, and use of said new substituted indazoles to produce drugs
Bayer Pharma Aktiengesellschaft
Indazolecarboxamides, processes for their preparation, pharmaceutical preparations comprising them and their use for producing medicaments
Bayer Pharma Aktiengesellschaft
Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors
Bristol-Myers Squibb
Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases
Biogen Ma
Heteroaryl substituted pyridyl compounds useful as kinase modulators
Bristol-Myers Squibb
Bicyclic heterocycle substituted pyridyl compounds useful as kinase modulators
Bristol-Myers Squibb
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Novartis Institutes For Biomedical Research
Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
Merck Sharp & Dohme
Heterocyclic-substituted pyridyl compounds useful as kinase inhibitors
Bristol-Myers Squibb
Amidopyrazole inhibitors of interleukin receptor-associated kinases
Merck Sharp & Dohme
Fluorescence Linked Enzyme Chemoproteomic Strategy for Discovery of a Potent and Selective DAPK1 and ZIPK Inhibitor.
Duke University Medical Center
A Hexylchloride-Based Catch-and-Release System for Chemical Proteomic Applications.
University of Washington
Affinity reagents that target a specific inactive form of protein kinases.
University of Washington
Heteroaryl substituted pyridyl compounds useful as kinase modulators
Bristol-Myers Squibb