186 articles for X Huang
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Phloroglucinol Derivatives with Protein Tyrosine Phosphatase 1B Inhibitory Activities from Eugenia jambolana Seeds.
Northeastern University
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Amgen
Discovery of Potent and Selective Agonists ofd Opioid Receptor by Revisiting the"Message-Address" Concept.
Fudan University
Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis.
Southeast University
Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.
China Pharmaceutical University
Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.
Amgen
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.
Amgen
Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.
Purdue University
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
Amgen
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Amgen
cis-1-Oxo-heterocyclyl-4-amido cyclohexane derivatives as NPY5 receptor antagonists.
Lundbeck Research Usa
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Amgen
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
Lundbeck Research Usa
Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Amgen
Development of oleanane-type triterpenes as a new class of HCV entry inhibitors.
Peking University
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Merck Research Laboratories
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.
Merck Research Laboratories
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
University of Arkansas For Medical Sciences
Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.
Amgen
The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.
Merck Research Laboratory
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
Chinese Academy of Sciences
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
Amgen
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.
Purdue University
Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Vanderbilt University Medical Center
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1¿) inhibitors.
Amgen
Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potentß-secretase inhibitors.
Purdue University
Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Ka and mTOR.
Pfizer
Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.
TBA
Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.
TBA
Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.
TBA
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.
TBA
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.
Zhejiang University
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
University of Kentucky
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.
Amgen
Synthesis and monoamine transporter binding properties of 2,3-cyclo analogues of 3beta-(4'-aminophenyl)-2beta-tropanemethanol.
Research Triangle Institute
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
Amgen
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious¿-secretase modulators in vivo.
Schering-Plough Research Institute
SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist.
Merck Research Laboratory
Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.
Merck Research Laboratories
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Merck Research Laboratories
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.
Amgen
New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.
Chinese Academy of Sciences
Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.
Research Triangle Institute
Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
Amgen
Discovery of a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia
TBA
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.
Pfizer
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Amgen
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Barrow Neurological Institute
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
Amgen
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Amgen
Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening.
Wyeth Pharmaceuticals
Discovery of X10g as a selective PROTAC degrader of Hsp90α protein for treating breast cancer.
Fujian Medical University (FMU)
Discovery of CZL-046 with an (S)-3-Fluoropyrrolidin-2-one Scaffold as a p300 Bromodomain Inhibitor for the Treatment of Multiple Myeloma.
Fudan University
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.
Sun Yat-Sen University
Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment.
Central South University
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
Sun Yat-Sen University
Hit-to-Lead Optimization of Heterocyclic Carbonyloxycarboximidamides as Selective Antagonists at Human Adenosine A3 Receptor.
University of Cambridge
Structure-based discovery of a new series of nucleoside-derived ring-opening PRMT5 inhibitors.
University of Chinese Academy of Sciences
Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma.
Fudan University
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Kymera Therapeutics
Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases.
Hangzhou Medical College
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.
Sichuan University
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery.
Shandong University
Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agents.
Yale University
Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives.
Sichuan University
Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.
Sun Yat-Sen University
Discovery of a potent and selective proteolysis targeting chimera (PROTAC) degrader of NSD3 histone methyltransferase.
Shanghai Institute of Materia Medica
Modes of action insights from the crystallographic structures of retinoic acid receptor-related orphan receptor-γt (RORγt).
Fudan University
Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
Amgen
Development and therapeutic potential of adaptor-associated kinase 1 inhibitors in human multifaceted diseases.
Sichuan Univiersity
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Shanghai Jiao Tong University
Novel combretastatin A-4 derivative containing aminophosphonates as dual inhibitors of tubulin and matrix metalloproteinases for lung cancer treatment.
Huaiyin Institute of Technology
Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy.
Shanghai Institute of Materia Medica
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Amgen
Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5.
Sun Yat-Sen University
Discovery of dual-target ligands binding to beta2-adrenoceptor and cysteinyl-leukotriene receptor for the potential treatment of asthma from natural products derived DNA-encoded library.
Northwest University
Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.
Anhui Medical University
Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer.
Fujian Medical University (Fmu)
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.
Chinese Academy of Sciences
Discovery of novel benzimidazole derivatives as potent p300 bromodomain inhibitors with anti-proliferative activity in multiple cancer cells.
Fudan University
Telocinobufagin Has Antitumor Effects in Non-Small-Cell Lung Cancer by Inhibiting STAT3 Signaling.
Wenzhou Medical University
Discovery and Structure-Activity Relationship Studies of Novel Adenosine A
University of Bern
Design, synthesis, and structure-activity relationship of PD-1/PD-L1 inhibitors with a benzo[d]isoxazole scaffold.
Peking Union Medical College
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
Merck
Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship,
Northeastern University
5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma.
Chinese Academy of Sciences
Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold.
Peking Union Medical College
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
Anhui Medical University
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR
Zhengzhou University
Molecular docking and 3D-QSAR studies on gag peptide analogue inhibitors interacting with human cyclophilin A.
Chinese Academy of Sciences
Synthesis and identification of a novel derivative of salidroside as a selective, competitive inhibitor of monoamine oxidase B with enhanced neuroprotective properties.
Fujian University of Traditional Chinese Medicine
Synthesis and Metabolism of BTN3A1 Ligands: Studies on Modifications of the Allylic Alcohol.
University of Iowa
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models.
Chinese Academy of Sciences
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities.
Fujian Medical University (Fmu)
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of novel human monoamine oxidase B inhibitors based on a fragment in an X-ray crystal structure.
Hefei University of Technology
Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia.
Chinese Academy of Sciences
Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3.
Guangxi Normal University
Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
Fudan University
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
TBA
Novel Pyrazolo[4,3- d]pyrimidine as Potent and Orally Active Inducible Nitric Oxide Synthase (iNOS) Dimerization Inhibitor with Efficacy in Rheumatoid Arthritis Mouse Model.
Anhui Medical University
Development of the First Low Nanomolar Liver Receptor Homolog-1 Agonist through Structure-guided Design.
Emory University School of Medicine
Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors.
Hefei University of Technology
Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.
Peking University
1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist.
Purdue University
Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.
Zhejiang University
Subnanomolar inhibitor of cytochrome bc1 complex designed by optimizing interaction with conformationally flexible residues.
Central China Normal University
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Merck Research Laboratory
Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.
Merck Research Laboratories
Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.
National Center For Advancing Translational Sciences
Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand.
Purdue University
Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.
Merck Research Laboratory
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Abbvie
The synthesis of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as potent CRTh
Merck
Design, synthesis, and biological activity of 5'-phenyl-1,2,5,6-tetrahydro-3,3'-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.
University of Michigan
Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators.
Merck Research Laboratories
Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
China Pharmaceutical University
A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.
China Pharmaceutical University
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Abbvie
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Abbvie
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.
Purdue University
1,2,3',5'-tetrahydro-2'h-spiro[indole-3,1'-pyrrolo[3,4-C]pyrrole]-2,3'-dione compounds as therapeutic agents activating TP53
Adamed Pharma
FAK DEGRADERS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC APPLICATIONS
Berrybio (Shanghai)
METHIONINE ADENOSYLTRANSFERASE 2A HETEROCYCLIC INHIBITOR
Nanjing Chia Tai Tianqing Pharmaceutical Co.
Polycyclic carbamoylpyridone derivatives, pharmaceutical compositions and use thereof
Jiaxing Andicon Biotech Co.
Compounds for the modulation of cyclophilins function
The University Court of The University of Edinburgh
Oxadiazaspiro compounds for the treatment of drug abuse and addiction
Esteve Pharmaceuticals.
Benzenesulfonamide compounds and their use as therapeutic agents
Xenon Pharmaceuticals
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma
[1,2,3]triazolo[4,5-D]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor
Hoffmann-La Roche
Sulfoximine substituted quinazolines for pharmaceutical compositions
Evotec International
Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
University of Oxford
Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.
Vanderbilt University
Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy
Abbvie Deutschland
Inhibition of arginine aminopeptidase by bestatin and arphamenine analogues. Evidence for a new mode of binding to aminopeptidases.
University of Wisconsin
A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis.
Nagoya University School of Medicine
Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen.
Manchester Interdisciplinary Biocentre
Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.
Mcgill University
Cloning and characterization of the human GABAA receptor alpha 4 subunit: identification of a unique diazepam-insensitive binding site.
Cocensys
Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
U. 109
Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Burnham Institute For Medical Research
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
Eli Lilly