230 articles for J Wu
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Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect isletβ-cells from apoptosis.
East China Normal University
Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
South China University of Technology
Design, synthesis and biological evaluation of novel non-peptide boronic acid derivatives as proteasome inhibitors.
China Pharmaceutical University
Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer.
Wenzhou Medical Universtiy
Modulatory effects of silibinin in various cell signaling pathways against liver disorders and cancer - A comprehensive review.
Tasly Pharmaceutical Group
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
China Pharmaceutical University
Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.
Whitman College
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.
Genentech
Potentµ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
Torrey Pines Institute For Molecular Studies
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Chinese Academy of Sciences
Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO).
Zhengzhou University
Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5).
Merck Research Laboratories
Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6).
Merck Research Laboratories
Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University)
Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).
Merck Research Laboratories
Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.
University of Maryland
Rapid development of two factor IXa inhibitors from hit to lead.
Merck Research Laboratories
Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4).
Merck Research Laboratories
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Merck Research Laboratories
Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5.
University of Maryland
Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.
China Pharmaceutical University
Structure-activity relationship and interaction studies of new SIRT1 inhibitors with the scaffold of 3-(furan-2-yl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole.
Chinese Academy of Sciences
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.
TBA
Discovery of potent KIFC1 inhibitors using a method of integrated high-throughput synthesis and screening.
Astrazeneca
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.
Merck Research Laboratories
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Forma Therapeutics
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Merck
Discovery of a potent and selectivea3ß4 nicotinic acetylcholine receptor antagonist from ana-conotoxin synthetic combinatorial library.
Torrey Pines Institute For Molecular Studies
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Merck Research Laboratories
Discovery of MK-7655, aß-lactamase inhibitor for combination with Primaxin®.
Merck Research Labs
Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.
Torrey Pines Institute For Molecular Studies
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.
Zhejiang University
Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.
Astrazeneca
Discovery and mechanism study of SIRT1 activators that promote the deacetylation of fluorophore-labeled substrate.
Chinese Academy of Sciences
Identification of benzofuran-3-yl(phenyl)methanones as novel SIRT1 inhibitors: binding mode, inhibitory mechanism and biological action.
Chinese Academy of Sciences
Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
Genentech
Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47.
TBA
Synthesis and structure-activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1).
Activx Biosciences
Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKe kinases.
Astrazeneca R&D Boston
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry.
Duquesne University
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part II).
Shandong University
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).
Shandong University
Crystal structures of Saccharomyces cerevisiae N-myristoyltransferase with bound myristoyl-CoA and inhibitors reveal the functional roles of the N-terminal region.
Chinese Academy of Sciences
Disruption of Kv1.1 N-type inactivation by novel small molecule inhibitors (disinactivators).
Wyeth Research
Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series.
Merck Frosst Centre For Therapeutic Research
Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases.
Institute of The Sir Mortimer Jewish General Hospital
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Pfizer
6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site.
University of Groningen
Side chain SAR of bicyclicß-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.
Merck Research Labs
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.
Genomics Institute of The Novartis Research Foundation
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.
Merck Frosst Centre For Therapeutic Research
Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.
Genentech
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Merck Frosst Centre For Therapeutic Research
Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
H. Lee Moffitt Cancer Center and Research Institute
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Elan Pharmaceuticals
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Elan Pharmaceuticals
The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.
Merck Research Laboratories
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem.
Merck Research Labs
3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.
Wyeth Research
Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.
Activx Biosciences
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma.
Wyeth Research
Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry.
Wayne State University School of Medicine
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?
Pfizer
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.
Roche Palo Alto
Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: design, synthesis and antifolate activity.
Peking University
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Merck Research Laboratories
Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects.
Activx Biosciences
A highly selective dual insulin receptor (IR)/insulin-like growth factor 1 receptor (IGF-1R) inhibitor derived from an extracellular signal-regulated kinase (ERK) inhibitor.
Fox Chase Cancer Center
Development of novel celastrol-ligustrazine hybrids as potent peroxiredoxin 1 inhibitors against lung cancer.
Anhui University of Science and Technology
Development of Nitric Oxide-Donating Netarsudil Derivatives as a Synergistic Therapy for Glaucoma with Reduced Ocular Irritation.
China Pharmaceutical University
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Wyeth Research
Design, synthesis, and biological evaluation of aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.
Shanghai Institute of Pharmaceutical Industry Co., Ltd.
Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer.
Guizhou Medical University
Structure-activity relationship study of 1,6-naphthyridinone derivatives as selective type II AXL inhibitors with potent antitumor efficacy.
University of South China
Advances in nitric oxide regulators for the treatment of ischemic stroke.
China Pharmaceutical University
Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7.
Tianjin University
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Merck & Co.
Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.
Elan Pharmaceuticals
Current advances and development strategies of targeting son of sevenless 1 (SOS1) in drug discovery.
Sichuan University
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.
Wyeth Research
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.
Insilico Medicine Shanghai
Covalent Peptide LSD1 Inhibitor Specifically Recognizes Cys360 in the Enzyme-Active Region.
Shenzhen University
Design, Synthesis, and Biological Evaluation of Proteolysis-Targeting Chimeras as Highly Selective and Efficient Degraders of Extracellular Signal-Regulated Kinase 5.
Peking University
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Abbott Laboratories
Novel Amphibian Bowman-Birk-Like Inhibitor with Antioxidant and Anticoagulant Effects Ameliorates Pancreatitis Symptoms in Mice.
Southern Medical University
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
Schering-Plough Research Institute
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Merck Research Laboratories
Overview of CFTR activators and their recent studies for dry eye disease: a review.
Shenyang Pharmaceutical University
Synthesis and biological evaluation of diamine-based histamine H3 antagonists with serotonin reuptake inhibitor activity.
Johnson & Johnson Pharmaceutical Research & Development
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
Nurix Therapeutics
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway.
Peking University
Discovery of NXT-10796, an orally active, intestinally restricted EP4 agonist prodrug for the treatment of inflammatory bowel disease.
Inception Sciences Canada
Discovery of Novel PTP1B Inhibitors with Once-Weekly Therapeutic Potential for Type 2 Diabetes: Design, Synthesis, and
Qingdao University
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Merck
Design, synthesis, and biological evaluation of novel N-Benzyl piperidine derivatives as potent HDAC/AChE inhibitors for Alzheimer's disease.
Shandong University
Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.
South China University of Technology
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
Merck
Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
Nanjing Chia-Tai Tianqing Pharmaceutical
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism.
Peking Union Medical College
Chemical synthesis and pharmacological properties of heparin pentasaccharide analogues.
Chinese Academy of Sciences
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.
Southern Medical University Biomedical Research Center
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Janssen Research & Development
Identification of Antithrombotic Natural Products Targeting the Major Substrate Binding Pocket of Protein Disulfide Isomerase.
Fuzhou University
Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities.
Sun Yat-Sen University
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
Schering-Plough Research Institute
Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP.
Baylor College of Medicine
Synthesis and evaluation of inhibitors of Mycobacterium tuberculosis UGM using bioisosteric replacement.
Guizhou University of Traditional Chinese Medicine
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.
Schering-Plough Research Institute
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
University of Science and Technology of China
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Bristol-Myers Squibb
Bradykinin-Potentiating Peptide-Paclitaxel Conjugate Directed at Ectopically Expressed Angiotensin-Converting Enzyme in Triple-Negative Breast Cancer.
Hong Kong Baptist University
Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer.
Nanjing University of Chinese Medicine
Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.
South China University of Technology
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Merck Research Laboratories
Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70.
St. Jude Children'S Research Hospital
Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
Anhui Medical University
Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Tianjin University of Traditional Chinese Medicine
Dual Glycolate Oxidase/Lactate Dehydrogenase A Inhibitors for Primary Hyperoxaluria.
Chinook Therapeutics
Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
Janssen Research & Development
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 macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Merck
Synthesis, Structure-Activity Relationships, and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease.
Baylor College of Medicine
Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer.
Wenzhou Medical University
Discovery of a novel chimeric ubenimex-gemcitabine with potent oral antitumor activity.
Shandong University
Fluoro analogs of bioactive oxy-sterols: Synthesis of an EBI2 agonist with enhanced metabolic stability.
Janssen Research & Development
Discovery of Novel PTP1B Inhibitors Derived from the BH3 Domain of Proapoptotic Bcl-2 Proteins with Antidiabetic Potency.
Qingdao University of Science and Technology
Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.
Roche Innovation Center Shanghai
Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors.
Astrazeneca
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Merck
Inhibition of cholesteryl ester synthesis by polyacetylenes from Atractylodes rhizome.
Kitasato University
Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
Jinan University
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Merck
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Merck
Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.
TBA
Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors.
Shandong University
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.
High Magnetic Field Laboratory
Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.
Genentech
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Genomics Institute of The Novartis Research Foundation (Gnf)
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Chinese Academy of Sciences
Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC.
Wuxi Shuangliang Biotechnology
Design, synthesis, and screening of novel ursolic acid derivatives as potential anti-cancer agents that target the HIF-1α pathway.
Yanbian University College of Pharmacy
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).
Idun Pharmaceuticals
Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP.
Avera Institute For Human Genetics
Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
Beijing University of Chemical Technology
Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.
St. Jude Children'S Research Hospital
Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases.
Shandong University
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Astrazeneca
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Shandong University
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).
Elan Pharmaceuticals
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Elan Pharmaceuticals
Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.
Chinese Academy of Sciences
Novel 8-hydroxyquinoline derivatives targeting β-amyloid aggregation, metal chelation and oxidative stress against Alzheimer's disease.
Pharmaceutical University
Structure optimization and preliminary bioactivity evaluation of N-hydroxybenzamide-based HDAC inhibitors with Y-shaped cap.
Shandong University
New MD2 inhibitors derived from curcumin with improved anti-inflammatory activity.
Wenzhou Medical University
Docking based design of diastereoisomeric MTCA as GPIIb/IIIa receptor inhibitor.
Capital Medical University
Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors.
The First Affiliated Hospital of Wenzhou Medical University
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC.
Chinese Academy of Sciences
Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.
Progenra
Design, synthesis and tumor cell growth inhibitory activity of 3-nitro-2H-cheromene derivatives as histone deacetylaes inhibitors.
Shandong University
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.
High Magnetic Field Laboratory
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.
Chinese Academy of Sciences
Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c fromα-Santonin Derivatives.
Second Military Medical University
Highly Selective and Potentα4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.
Torrey Pines Institute For Molecular Studies
Selective HDAC inhibitors with potent oral activity against leukemia and colorectal cancer: Design, structure-activity relationship and anti-tumor activity study.
Shandong University
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Moe) and Hubei Provinc
QUINAZOLINE COMPOUNDS AND USES THEREOF AS INHIBITORS OF MUTANT KRAS PROTEINS
Amgen
Substituted benzyl-triazole compounds for Cbl-b inhibition, and further uses thereof
Nurix Therapeutics
HETEROCYCLE-CONTAINING LONP1 INHIBITOR COMPOUNDS, USES AND METHODS
Pretzel Therapeutics
SPIROCYCLIC ANNULATED 2-AMINO-3-CYANO THIOPHENES AND DERIVATIVES FOR THE TREATMENT OF CANCER
Boehringer Ingelheim International
Azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
Hoffmann-La Roche
Polycyclic carbamoylpyridone derivatives, pharmaceutical compositions and use thereof
Jiaxing Andicon Biotech Co.
RING-MODIFIED PROLINE SHORT PEPTIDE COMPOUND AND USE THEREOF
Fujian Akeylink Biotechnology
1-ALKYL-5-ARYLIDENE-2-SELENOXOIMIDAZOLIDINE-4-ON AND DERIVATIVE THEREOF, PREPARATION METHOD THEREFOR, AND COMPOSITION COMPRISING SAME FOR PREVENTING, ALLEVIATING OR TREATING NEURODEGENERATIVE DISEASES
Duksung Women''S University Industry-Academic Cooperation Foundation
Indazole compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
Novartis
Synthesis, activity evaluation, and docking analysis of barbituric acid aryl hydrazone derivatives as RSK2 inhibitors.
East China University of Science and Technology
Simple methanesulfonates are hydrolyzed by the sulfatase carbonic anhydrase activity.
Agri Ibrahim Cecen University
Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
Genentech
Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library.
X-Chem Pharmaceuticals
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Novartis Institutes For Biomedical Research
Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
Advinus Therapeutics
Therapeutic compounds for blocking DNA synthesis of POX viruses
University of Pennsylvania
Amidopyrazole inhibitors of interleukin receptor-associated kinases
Merck Sharp & Dohme
Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
Boehringer Ingelheim International
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.
Dana-Farber Cancer Institute
Synthesis,MolecularModeling, and Biological Evaluation of Novel Tetrahydro-ß-Carboline Hydantoin and Tetrahydro-ß-Carboline Thiohydantoin Derivatives as Phosphodiesterase 5 Inhibitors
German University In Cairo
Combined X-ray, NMR, and kinetic analyses reveal uncommon binding characteristics of the hepatitis C virus NS3-NS4A protease inhibitor BI 201335.
Boehringer Ingelheim (Canada)
Ligand-directed functional heterogeneity of histamine H1 receptors: novel dual-function ligands selectively activate and block H1-mediated phospholipase C and adenylyl cyclase signaling.
University of North Carolina at Chapel Hill
Ligand specificity of nicotinic acetylcholine receptors in rat spinal cord: studies with nicotine and cytisine.
University of California
G protein-coupled receptor kinase 2 inhibitors and methods for use of the same
University of Michigan
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.
Santhera Pharmaceuticals
Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease.
National Defense Medical Center
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX.
Istituto Di Biostrutture E Bioimmagini-Cnr