121 articles for W Yang
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Article Title
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Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.
Sichuan University and Collaborative Innovation Center For Biotherapy
Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.
The Walter and Eliza Hall Institute of Medical Research
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors.
The Walter and Eliza Hall Institute of Medical Research
Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.
Bristol-Myers Squibb Research
Design, synthesis and biological evaluation of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine scaffold as DFG-out B-Raf kinase inhibitors.
China Pharmaceutical University
Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.
Bristol-Myers Squibb
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.
Chinese Academy of Sciences
Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors.
Bristol-Myers Squibb
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.
Chinese Academy of Sciences
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication.
Sanofi
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.
Genentech
Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.
Nanjing University
Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.
Merck Research Laboratories
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Maxim Pharmaceuticals
New inhibitor of 3-phosphoinositide dependent protein kinase-1 identified from virtual screening.
Central China Normal University
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Genzyme
Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Genzyme
Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Genzyme
Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
Genzyme
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Shanghai Hengrui Pharmaceuticals
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Shanghai Hengrui Pharmaceuticals
Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations.
Duke University
A Lysosome-Targeting hNEU1 Inhibitor Treats Myocardial Infarction: A Potential Therapeutic Breakthrough.
Southeast University
Design and synthesis of the first PARP-1 and proteasome dual inhibitors to treat breast cancer.
Sichuan University
Design, Synthesis and Antitumor Activity of a Novel Class of SHP2 Allosteric Inhibitors with a Furanyl Amide-Based Scaffold.
Shandong University
Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy.
Nanjing University of Chinese Medicine
RIPK1 inhibitors: A key to unlocking the potential of necroptosis in drug development.
Lanzhou University Second Hospital
Design, synthesis and biological evaluation of 2,4,6- trisubstituted triazine derivatives as new nonpeptide small-molecule SIRT5 inhibitors.
Xihua University
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.
China Pharmaceutical University
Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
Astrazeneca
Discovery of BRD4-HDAC Dual Inhibitors with Improved Fungal Selectivity and Potent Synergistic Antifungal Activity against Fluconazole-Resistant
East China University of Science & Technology
Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.
Sichuan University
Development of Alkylated Hydrazides as Highly Potent and Selective Class I Histone Deacetylase Inhibitors with T cell Modulatory Properties.
Martin-Luther University of Halle-Wittenberg
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.
China Pharmaceutical University
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis.
Hec Pharma.
Target-Based Virtual Screening and LC/MS-Guided Isolation Procedure for Identifying Phloroglucinol-Terpenoid Inhibitors of SARS-CoV-2.
Kunming Institute of Botany
Occurrence, synthesis and biological activity of 2-(2-phenyethyl)chromones.
Guizhou Medical University
The protective effects of natural product tunicatachalcone against neuroinflammation via targeting RIPK2 in microglia BV-2 cells stimulated by LPS.
Hebei Medical University
Discovery of 2-vinyl-10H-phenothiazine derivatives as a class of ferroptosis inhibitors with minimal human Ether-a-go-go related gene (hERG) activity for the treatment of DOX-induced cardiomyopathy.
Sichuan University
Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Biogen
Targeted Covalent Inhibition of Small CTD Phosphatase 1 to Promote the Degradation of the REST Transcription Factor in Human Cells.
University of California San Diego
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.
Maxim Pharmaceuticals
Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6
Sichuan University
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Bristol Myers Squibb
Design, synthesis and biological activities of benzo[d]imidazo[1,2-a]imidazole derivatives as TRPM2-specfic inhibitors.
Peking University
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
Peking University
Structure-Based Optimization of Quinazolines as Cruzain and
Federal University of Minas Gerais (Ufmg)
Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D.
Nankai University
Regulation of gene expression by synthetic dimerizers with novel specificity.
Ariad Gene Therapeutics
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
Structure-activity relationship studies of phenothiazine derivatives as a new class of ferroptosis inhibitors together with the therapeutic effect in an ischemic stroke model.
Sichuan University
Hydrogen Peroxide Inducible JAK3 Covalent Inhibitor: Prodrug for the Treatment of RA with Enhanced Safety Profile.
China Pharmaceutical University
The discovery, design and synthesis of potent agonists of adenylyl cyclase type 2 by virtual screening combining biological evaluation.
Chinese Academy of Sciences
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Astrazeneca
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Bristol Myers Squibb
Discovery of a potent and selective adenylyl cyclase type 8 agonist by docking-based virtual screening.
Kunming Medical University
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.
Roche Innovation Center Shanghai
Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket.
Ariad Gene Therapeutics
Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.
Monash University
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Bristol-Myers Squibb
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.
Biogen
Triazole-Based Inhibitors of the Wnt/β-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice.
University of Maryland
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.
Bristol-Myers Squibb
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
A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.
Shenyang Pharmaceutical University
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors.
Peking University
Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.
Genentech
Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.
Bristol-Myers Squibb
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.
Genentech
Potential anti-gout constituents as xanthine oxidase inhibitor from the fruits of Stauntonia brachyanthera.
Shenyang Pharmaceutical University
Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration.
Astrazeneca
PLPRO PROTEIN INHIBITOR, AND PREPARATION METHOD AND APPLICATION THEREOF
Tsinghua University
Isoindolinone substituted indoles and derivatives as RAS inhibitors
Boehringer Ingelheim International
FGFR4 inhibitor, preparation method therefor, and applications thereof
Jiangsu Hansoh Pharmaceutical Group
2-quinolone derived inhibitors of BCL6
The Institute of Cancer Research: Royal Cancer Hospital
4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as AOC3 inhibitors
Boehringer Ingelheim International
2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof
Shanghai Haiyan Pharmaceutical Technology
Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
Forma Therapeutics
Metabotropic glutamate receptor positive allosteric modulators (PAMS) and uses thereof
Sanford-Burnham Medical Research Institute
Substituted indazole derivatives active as kinase inhibitiors
Nerviano Medical Sciences
Heterocyclic derivatives and their use in the treatment of neurological disorders
Novartis
In vitro effects of cinnamic acid derivatives on protein tyrosine phosphatase 1B.
Chulalongkorn University
Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitors
Taibah University
Structure-Activity Relationships of Benzenesulfonamide-Based Inhibitors towards Carbonic Anhydrase Isoform Specificity.
University of Florida
Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
Boehringer Ingelheim International
Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Boehringer Ingelheim International
Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions
Boehringer Ingelheim International
Phosphorylated hydroxyethylamines as novel inhibitors of the bacterial cell wall biosynthesis enzymes MurC to MurF.
University of Ljubljana
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.
University of Toronto
7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity.
Third Tokushima Institute of New Drug Research
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes.
National Institute of Mental Health
Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist.
UniversitÉ
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.
Weizmann Institute of Science