118 articles for thisTarget
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Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors.
Takeda California
Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277.
Korea University
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Boehringer Ingelheim Rcv
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
Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-ß type I receptor kinase.
Ewha Womans University
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Massachusetts Institute of Technology
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.
Ewha Womans University
4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-ß type I receptor kinase.
Ewha Womans University
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles as inhibitors of transforming growth factor-ß type I receptor (ALK5).
Capital Normal University
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Vanderbilt University Medical Center
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Glaxosmithkline
Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-ß type 1 receptor kinase inhibitors.
Ewha Womans University
5-(1,3-Benzothiazol-6-yl)-4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazole derivatives as potent and selective transforming growth factor-ß type I receptor inhibitors.
Taisho Pharmaceutical
Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFß signaling.
Human Biomolecular Research Institute
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring.
Pfizer
Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-ß type 1 receptor kinase inhibitors.
Ewha Womans University
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
Glaxosmithkline
Design, synthesis, and evaluation of novel 4-thiazolylimidazoles as inhibitors of transforming growth factor-ß type I receptor kinase.
Taisho Pharmaceutical
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Glaxosmithkline
Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-ß type 1 receptor kinase inhibitors.
Ewha Womans University
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Glaxosmithkline
Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.
Ewha Womans University
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Glaxosmithkline
Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI).
Boehringer Ingelheim Pharma
Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Ewha Womans University
3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists.
Northeastern Ohio Universities Colleges of Medicine and Pharmacy
Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-beta type I receptor (ALK5) inhibitors.
Sichuan University
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).
Institute of Pharmacology and Toxicology
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors.
Glaxosmithkline
Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.
Glaxosmithkline
Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: novel selective inhibitors of transforming growth factor-beta kinase.
Kirin Pharma
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
Glaxosmithkline
Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Ewha Womans University
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Galapagos
Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.
Tibotec
Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening.
Baylor College of Medicine
Recent advances in small molecule based cancer immunotherapy.
Southern Medical University
Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d
Sungkyunkwan University
Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2.
Johann Wolfgang Goethe-University
Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage.
Minzu University of China
Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization.
Integral Biosciences
Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
University of Nimes
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Eli Lilly
Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors.
China Pharmaceutical University
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Incyte
Discovery of a novel 2-aminopyrazine-3-carboxamide as a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2) for the treatment of fibrodysplasia ossificans progressiva.
Novartis Institutes For Biomedical Research
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.
Glaxosmithkline
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
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.
Glaxosmithkline
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI).
Biogen
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Eli Lilly
Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors.
China Pharmaceutical University
Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors.
Yanbian University
Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.
Vanderbilt University
Discovery of Selective Transforming Growth Factor β Type II Receptor Inhibitors as Antifibrosis Agents.
Japan Tobacco
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
Glaxosmithkline
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ontario Institute For Cancer Research
Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-β (TGF-β) type I receptor inhibitors.
China Pharmaceutical University
Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5.
Yanbian University
Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors.
Yanbian University
Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.
Takeda California
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
University of Toronto
Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agent Targeting Transforming Growth Factor β Type I Receptor.
Sun Yat-Sen University
Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives.
Yanbian University
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Bristol-Myers Squibb Research & Development
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 Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.
Glaxosmithkline
ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles.
Palack£
Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.
Bristol-Myers Squibb Research and Development
Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.
National Center For Advancing Translational Sciences
Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
Institute of Cancer Research
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).
Bristol-Myers Squibb
Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor.
University of Toronto
Multi-targeted tyrosine kinase inhibitors effective in antitumor uses
Shanghai AB Pharmatech
TRIAZOLYL-METHYL SUBSTITUTED ALPHA-D-GALACTOPYRANOSIDE DERIVATIVES
Idorsia Pharmaceuticals
6-membered heterocyclic derivatives and pharmaceutical composition comprising the same
Shionogi
Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL
Cleveland Clinic
Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors
Valo Early Discovery
2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
Gilead Pharmasset
Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.
Hanoi University of Pharmacy
Synthesis, anti-inflammatory, analgesic, 5-lipoxygenase (5-LOX) inhibition activities, and molecular docking study of 7-substituted coumarin derivatives.
Nirma University
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.
Yogi Vemana University
Synthesis, Biological Evaluation, and Docking of Dihydropyrazole Sulfonamide Containing 2-hydroxyphenyl Moiety: A Series of Novel MMP-2 Inhibitors.
Nanjing University
Diversity-oriented fluorescence library approach (DOFLA) to the discovery of chymotrypsin sensor.
New York University
Thiazole derivatives as inhibitors of purified bovine liver mitochondrial monoamine oxidase-B: structure-activity relationships and theoretical study.
University of Catania
Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.
Sanofi Recherche
Design, synthesis, and characterization of new embelin derivatives as potent inhibitors of X-linked inhibitor of apoptosis protein.
University of Michigan