120 articles for Y Feng
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Merck
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
Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists.
Shanghai Institute of Materia Medica
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent.
Biomarin Pharmaceutical
Discovery of bis-aryl urea derivatives as potent and selective Limk inhibitors: Exploring Limk1 activity and Limk1/ROCK2 selectivity through a combined computational study.
Shanghai Institute of Technology
Tyrosyl-DNA Phosphodiesterase I Inhibitors from the Australian Plant Macropteranthes leichhardtii.
Griffith University
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.
Translational Research Institute
Discovery of Intestinal Targeted TGR5 Agonists for the Treatment of Type 2 Diabetes.
Chinese Academy of Sciences
Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.
Translational Research Institute
Discovery of potent and selective urea-based ROCK inhibitors: Exploring the inhibitor's potency and ROCK2/PKA selectivity by 3D-QSAR, molecular docking and molecular dynamics simulations.
Shanghai Institute of Technology
Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives.
Translational Research Institute
4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists.
Chinese Academy of Sciences
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Forma Therapeutics
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Genentech
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
Chinese Academy of Sciences
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Glaxosmithkline
Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.
Novartis Institutes For Biomedical Research
Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Novartis Institutes For Biomedical Research
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.
The Scripps Research Institute
Amino acid derived quinazolines as Rock/PKA inhibitors.
Translational Research Institute
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
Columbia University
Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach.
Dalian University of Technology
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Chinese Academy of Sciences
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.
Dalian University of Technology
An anthraquinone scaffold for putative, two-face Bim BH3a-helix mimic.
Dalian University of Technology
Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists.
Chinese Academy of Sciences
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Georgia State University
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Glaxosmithkline
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.
TBA
Synthesis and evaluation of carbocyanine dyes as PRMT inhibitors and imaging agents.
Georgia State University
Ianthellamide A, a selective kynurenine-3-hydroxylase inhibitor from the Australian marine sponge Ianthella quadrangulata.
Griffith University
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Novartis Institutes For Biomedical Research
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Chinese Academy of Sciences
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Chinese Academy of Sciences
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
Merck Research Laboratories
Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).
The Scripps Research Institute
Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).
The Scripps Research Institute
C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Chinese Academy of Sciences
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Glaxosmithkline
Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.
Translational Research Institute
Mycobacterium tuberculosis dihydrofolate reductase is not a target relevant to the antitubercular activity of isoniazid.
Texas A&M University
Discovery and mechanistic study of a class of protein arginine methylation inhibitors.
Georgia State University
Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro.
Harvard Medical School
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
The Scripps Research Institute
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators.
Chinese Academy of Sciences
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Chinese Academy of Sciences
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Merck Research Laboratories
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors.
Translational Research Institute and Department of Molecular Therapeutics
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Merck Research Laboratories
Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.
Institute For Medical Research
O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.
Pharmacy School of Wenzhou Medical College
Discovery of potent non-urea inhibitors of soluble epoxide hydrolase.
Columbia University
Discovery of novel small molecule cell type-specific enhancers of NF-kappaB nuclear translocation.
Columbia University
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
The Scripps Research Institute-Florida
Clavatadine A, a natural product with selective recognition and irreversible inhibition of factor XIa.
Griffith University
Development of novel antivrial agents that induce the degradation of the main protease of human-infecting coronaviruses.
Chinese Academy of Sciences
Potent, Selective, and Orally Bioavailable Quinazoline-Based STK17A/B Dual Inhibitors.
University of Miami Miller School of Medicine
Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.
China Pharmaceutical University
Vanillic acid derivatives from the green algae Cladophora socialis as potent protein tyrosine phosphatase 1B inhibitors.
Griffith University
Glycan-Modified Peptides for Dual Inhibition of Human Immunodeficiency Virus Entry into Dendritic Cells and T Cells.
Chinese Academy of Sciences
Discovery of N-alkyl-N-benzyl thiazoles as novel TRPC antagonists for the treatment of glioblastoma multiforme.
Yantai University
The location, physiology, pathology of hippocampus Melatonin MT2 receptor and MT2-selective modulators.
The First Affiliated Hospital of China Medical University
Covalent Peptide LSD1 Inhibitor Specifically Recognizes Cys360 in the Enzyme-Active Region.
Shenzhen University
Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.
The Scripps Research Institute
Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.
Northwest University
A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion.
University of Miami
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Merck Research Laboratories
N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation.
Lanzhou University
-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors.
Reaction Biology
Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity.
China Pharmaceutical University
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
Chinese Academy of Sciences
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors.
Reaction Biology
Research advances on selective phosphatidylinositol 3 kinase δ (PI3Kδ) inhibitors.
Xi'An Jiaotong University
Computer-aided discovery of phenylpyrazole based amides as potent S6K1 inhibitors.
Shanghai Institute of Technology
Targeting the Allosteric Pathway That Interconnects the Core-Functional Scaffold and the Distal Phosphorylation Sites for Specific Dephosphorylation of Bcl-2.
Dalian University of Technology
Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation.
Lanzhou University
Switching a Xanthine Oxidase Inhibitor to a Dual-Target Antagonist of P2Y
Shenyang Pharmaceutical University
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
TBA
Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.
Sun Yat-Sen University
Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors.
Northwest A&F University
Discovery of (S)-6-methoxy-chroman-3-carboxylic acid (4-pyridin-4-yl-phenyl)-amide as potent and isoform selective ROCK2 inhibitors.
Shanghai Institute of Technology
Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors.
Xi'An Jiaotong University
Bioactivatable Pseudotripeptidization of Cyclic Dipeptides To Increase the Affinity toward Oligopeptide Transporter 1 for Enhanced Oral Absorption: An Application to Cyclo(l-Hyp-l-Ser) (JBP485).
Dalian Medical University
A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.
China Pharmaceutical University
Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.
Yantai University
Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).
Mcgill University
SAR Exploration of Tight-Binding Inhibitors of Influenza Virus PA Endonuclease.
University of California
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
Dalian University of Technology
Identification of a potent inhibitor targeting human lactate dehydrogenase A and its metabolic modulation for cancer cell line.
Chongqing University
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.
Xi'An Jiaotong University
Design, synthesis and biological evaluation of 1-hydroxy-2-phenyl-4-pyridyl-1H-imidazole derivatives as xanthine oxidase inhibitors.
Shenyang Pharmaceutical University
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors.
Xi'An Jiaotong University
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities.
Chinese Academy of Sciences
Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.
Guangdong Pharmaceutical University
Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.
Hebei University
Achyrodimer F, a tyrosyl-DNA phosphodiesterase I inhibitor from an Australian fungus of the family Cortinariaceae.
Griffith University
3-amino-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of MRGX2
Solent Therapeutics
COMPOSITIONS AND METHODS FOR TARGETED DEGRADATION OF PROTEINS IN A PLANT CELL
Oerth Bio
A high quality, industrial data set for binding affinity prediction: performance comparison in different early drug discovery scenarios.
F. Hoffmann-La Roche
Dopamine D3 receptor selective antagonists/partial agonists and uses thereof
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Method of treatment using substituted imidazo[1,2b]pyridazine compounds
Array Biopharma
Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands.
Yeditepe University