145 articles for D Chen
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.
Merck
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Design, synthesis and antithrombotic evaluation of novel non-peptide thrombin inhibitors.
China Pharmaceutical University
Cyclic peptide-based potent and selective SIRT1/2 dual inhibitors harboring N
Jiangsu University
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
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.
Glaxosmithkline
Design, synthesis and antithrombotic evaluation of novel dabigatran etexilate analogs, a new series of non-peptides thrombin inhibitors.
China Pharmaceutical University
Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.
Qilu Pharmaceutical
Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) Ministry of Education
Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization.
Shanghai Institute of Materia Medica
Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs.
Health Science Center Xi'An Jiaotong University
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors.
Chinese Academy of Sciences
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization.
Chinese Academy of Sciences
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Merck Research Laboratories
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.
Merck Research Laboratories
Discovery and mechanism study of SIRT1 activators that promote the deacetylation of fluorophore-labeled substrate.
Chinese Academy of Sciences
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymph
S*Bio
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
Roche R & D Center China
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arth
S Bio
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Amgen
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Amgen
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
Glaxosmithkline
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.
Glaxosmithkline
Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
S*Bio
Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity
TBA
1-(1-acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia.
Ar£Te Therapeutics
Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).
Berlex Biosciences
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
S*Bio
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.
National Center For Drug Screening
Discovery of tricyclic PARP7 inhibitors with high potency, selectivity, and oral bioavailability.
Hubei Polytechnic University
Serendipitous discovery of Class I HDAC inhibitors from rational design of molecular glue degraders targeting HDAC.
Guizhou Medical University
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
Kymera Therapeutics
Synthesis and Bioevaluation of 3-(Arylmethylene)indole Derivatives: Discovery of a Novel ALK Modulator with Antiglioblastoma Activities.
Nanjing Medical University
Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities.
Shanghai University
2,6-diazaspiro[3.4]octan-7-one derivatives as potent sigma-1 receptor antagonists that enhanced the antinociceptive effect of morphine and rescued morphine tolerance.
Xuzhou Medical University
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
Mirati Therapeutics
Allosteric Inhibitors of Macrophage Migration Inhibitory Factor (MIF) Interfere with Apoptosis-Inducing Factor (AIF) Co-Localization to Prevent Parthanatos.
University of Groningen
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Nanjing Medical University
Facilitated Drug Repurposing with Artemisinin-Derived PROTACs: Unveiling PCLAF as a Therapeutic Target.
Guizhou Medical University
Development of a series of quinazoline-2,5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Shanghai Institute of Materia Medica
Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.
Wayne State University
Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy.
Shanghai Institute of Materia Medica
Small molecule approaches to treat autoimmune and inflammatory diseases (Part III): Targeting cytokines and cytokine receptor complexes.
Roche Innovation Center Shanghai
Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.
Peking Union Medical College and Chinese Academy of Medical Sciences
Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
Nanjing Chia-Tai Tianqing Pharmaceutical
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.
Wenzhou Medical University
Discovery of 1-(Hetero)aryl-β-carboline Derivatives as IDO1/TDO Dual Inhibitors with Antidepressant Activity.
Nanjing Medical University
Design, synthesis and antitumor evaluation of novel 1H-indole-2-carboxylic acid derivatives targeting 14-3-3η protein.
Tsinghua University
Discovery and Evaluation of Novel Angular Fused Pyridoquinazolinonecarboxamides as RNA Polymerase I Inhibitors.
Johns Hopkins University
Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction.
China Pharmaceutical University
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.
Lanzhou University
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).
China Pharmaceutical University
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Merck
Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.
Fujian Medical University
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.
China Pharmaceutical University
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
Merck
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
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1
Chinese Academy of Sciences
Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.
Virginia Commonwealth University
Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF).
University of Groningen
Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).
University of Groningen
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
A*Star
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.
Lanzhou University
7-Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor.
University of Groningen
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1.
Purdue University
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.
Shanghai Institute of Materia Medica
Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.
Sun Yat-Sen University
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.
Shenyang Pharmaceutical University
Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues.
Purdue University
Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors.
Nanjing Medical University
Discovery of a potent and selective adenylyl cyclase type 8 agonist by docking-based virtual screening.
Kunming Medical University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Merck And
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.
University of Chinese Academy of Sciences
Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma.
Chinese Academy of Sciences
Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction.
Chinese Academy of Sciences
Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia.
Chinese Academy of Sciences
Discovery of Bisubstrate Inhibitors for Protein N-Terminal Methyltransferase 1.
Purdue University
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer.
Chinese Academy of Sciences
Exploring structure-activity relationships around the phosphomannose isomerase inhibitor AF14049 via combinatorial synthesis.
Affymax Research Institute
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.
University of Chinese Academy of Sciences
Targeting tropomyosin receptor kinase for cancer therapy.
China Pharmaceutical University
Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
TBA
Novel Propargyl-Linked Bisubstrate Analogues as Tight-Binding Inhibitors for Nicotinamide
TBA
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.
Glaxosmithkline
Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.
Abdulaziz University For Health Sciences
Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity.
Chia Tai Tianqing Pharmaceutical Group
NAD(P)H:Quinone Oxidoreductase 1 (NQO1) as a Therapeutic and Diagnostic Target in Cancer.
China Pharmaceutical University
Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
China Pharmaceutical University
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors.
Roche Innovation Center Shanghai
Design and optimization of purine derivatives as in vivo active PDE10A inhibitors.
Nanchang University
TREATMENT OF MYELOPROLIFERATIVE DISEASES AND DISORDERS WITH INHIBITORS OF BET FAMILY BDII BROMODOMAIN
Poseidon Innovation 1
SALT OF DIHYDROPYRIDO[2,3-D]PYRIMIDINONE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Nanjing Chia Tai Tianqing Pharmaceutical
Substituted pyrazolopyrazines, imidazopyrazines and [1,2,4]triazolopyrazines as allosteric SHP2 inhibitors
Revolution Medicines
Substituted pyrido[2,3-d]pyrimidines as inhibitors of Ras pathway signaling
Kumquat Biosciences
Polypeptide compound, pharmaceutical composition, preparation method and application thereof
Chengdu Sintanovo Biotechnology
Haloallylamine indole and azaindole derivative inhibitors of lysyl oxidases and uses thereof
Pharmaxis
Selective inhibitors of protein arginine methlytransferase 5 (PRMT5)
Prelude Therapeutics
Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure-Activity Relationship, and X-ray Structural Studies.
Purdue University
Potent and selective inhibitors of monoamine transporters; method of making; and use thereof
The United States of America, As Represented By The Secretary, Department of Health and Human Services
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl) oxy) napththalen-1-yl) ureas as P38 MAP knase inhibitors
Respivert
Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
Forma Tm2
Inhibition of the alpha- and beta-carbonic anhydrases from the gastric pathogen Helycobacter pylori with anions.
Universit�� Degli Studi Di Firenze
Mechanism of Flavoprotein l-6-Hydroxynicotine Oxidase: pH and Solvent Isotope Effects and Identification of Key Active Site Residues.
University of Texas Health Science Center
Novel structural and functional insights into M3 muscarinic receptor dimer/oligomer formation.
National Institutes of Health
Methods for increasing the stabilization of hypoxia inducible factor-α
Aerpio Therapeutics
Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2).
University of Michigan
The A128T resistance mutation reveals aberrant protein multimerization as the primary mechanism of action of allosteric HIV-1 integrase inhibitors.
The Ohio State University
Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds.
Moffitt Cancer Center
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Palacky University