48 articles for L Yan
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
Kbp Biosciences
Simple N(e)-thioacetyl-lysine-containing cyclic peptides exhibiting highly potent sirtuin inhibition.
Jiangsu University
Exploration of cyanine compounds as selective inhibitors of protein arginine methyltransferases: synthesis and biological evaluation.
The University of Georgia
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
The University of Georgia
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Georgia State University
Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor.
Bristol-Myers Squibb
Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors.
Nanjing University
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
Nanjing University
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Merck Research Laboratories
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Merck Research Laboratories
Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers.
Bristol-Myers Squibb Pharmaceutical Research and Development
Dihydropyrazolopyrimidines containing benzimidazoles as K(V)1.5 potassium channel antagonists.
Bristol-Myers Squibb
Allosteric Activation of Protein Phosphatase 5 with Small Molecules.
China Pharmaceutical University
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management.
Henan University
Identification of Piperazinyl-Difluoro-indene Derivatives Containing Pyridyl Groups as Potent FGFR Inhibitors against FGFR Mutant Tumor: Design, Synthesis, and Biological Evaluation.
Peking Union Medical College and Chinese Academy of Medical Sciences
Design, synthesis and antitumor activity of 4-arylamine substituted pyrimidine derivatives as noncovalent EGFR inhibitors overcoming C797S mutation.
Guizhou University
Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors.
Central South University
Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
Skyrun Pharma Co.
Discovery of a novel 1H-pyrazole- [3,4-b] pyridine-based lysine demethylase 5B inhibitor with potential anti-prostate cancer activity that perturbs the phosphoinositide 3-kinase/AKT pathway.
Zhengzhou University
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
University of Bonn
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Merck Research Laboratories
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Merck
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist.
Henan University
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Merck Research Laboratories
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
Discovery of Novel Orally Bioavailable Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo.
Tongji University
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
Mirati Therapeutics
Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines.
Eli Lilly
Design of Dimeric Bile Acid Derivatives as Potent and Selective Human NTCP Inhibitors.
National Institute of Biological Sciences
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
University of Bonn
Structure-Activity Relationships for the Marine Natural Product Sintokamides: Androgen Receptor N-Terminus Antagonists of Interest for Treatment of Metastatic Castration-Resistant Prostate Cancer.
Bc Cancer
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Eli Lilly
Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue.
National Institute of Biological Sciences
Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide.
Henan University
A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring N
Fudan University
Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists.
Henan University
Development of novel theranostic agents for in vivo amyloid imaging and protective effects on human neuroblastoma cells.
Guangdong University of Technology
Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1.
Henan University
Discovery of novel indirubin-3'-monoxime derivatives as potent inhibitors against CDK2 and CDK9.
Peking Union Medical College
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Agios Pharmaceuticals
Design, synthesis, and activity evaluation of novel erythropoietin mimetic peptides.
Beijing Institute of Pharmacology and Toxicology
USE OF GLYCOSYLTRASNFERASE INHIBITORS FOR TREATING CANCER
California Institute of Technology