225 articles for H Sun
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Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking.
The Ohio State University
Fragment-based discovery of novel pentacyclic triterpenoid derivatives as cholesteryl ester transfer protein inhibitors.
China Pharmaceutical University
Synthesis and biological evaluation of thiazole derivatives as novel USP7 inhibitors.
China Pharmaceutical University
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
Dalian Medical University
Modulatory effects of silibinin in various cell signaling pathways against liver disorders and cancer - A comprehensive review.
Tasly Pharmaceutical Group
Buried Hydrogen Bond Interactions Contribute to the High Potency of Complement Factor D Inhibitors.
University of Michigan
Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.
Bristol-Myers Squibb Research and Development
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea
Chinese Academy of Sciences
Polycyclic Polyprenylated Acylphloroglucinol Congeners from Hypericum scabrum.
Peking Union Medical College
Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.
China Pharmaceutical University
Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: introduction of an additional carboxyl group at the C-2 position of quinoline.
China Pharmaceutical University
Discovery of highly potent renin inhibitors potentially interacting with the S3' subsite of renin.
China Pharmaceutical University
Pseudosaccharin amines as potent and selective KV1.5 blockers.
Bristol-Myers Squibb Research and Development
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.
Pfizer
Phenolic Compounds from the Leaves and Twigs of Osteomeles schwerinae That Inhibit Rat Lens Aldose Reductase and Vessel Dilation in Zebrafish Larvae.
Institute of Oriental Medicine
Involvement of organic anion-transporting polypeptides in the hepatic uptake of dioscin in rats and humans.
Dalian Medical University
Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro/cyanobenzyl)-3-methyl-3,7-dihydro-purine-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors.
Southern Medical University
Design, synthesis and docking study of novel tetracyclic oxindole derivatives asa-glucosidase inhibitors.
Key Laboratory of Industrial Fermentation Microbiology (Tianjin University of Science and Technology)
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.
Chinese Academy of Sciences
Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.
Bristol-Myers Squibb Research and Development
Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
China Pharmaceutical University
Multitarget drug discovery for tuberculosis and other infectious diseases.
University of Illinois At Urbana-Champaign
Development of tag-free photoprobes for studies aimed at identifying the target of novel Group A Streptococcus antivirulence agents.
University of Michigan
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.
Jiangsu Aosaikang Pharmaceutical
Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Hoffmann-La Roche
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.
University of Michigan
Novel inhibitors of bacterial virulence: development of 5,6-dihydrobenzo[h]quinazolin-4(3H)-ones for the inhibition of group A streptococcal streptokinase expression.
University of Michigan
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
Chinese Academy of Sciences
Support vector machines classification of hERG liabilities based on atom types.
F. Hoffmann-La Roche
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
Pfizer
Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
University of Michigan
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
University of Michigan
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor.
Shenyang Pharmaceutical 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
Practical access to four stereoisomers of naftidrofuryl and their binding affinity towards 5-hydroxytryptamine 2A receptor.
China Pharmaceutical University
Practical synthesis of bredemolic acid, a natural inhibitor of glycogen phosphorylase.
China Pharmaceutical University
Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase.
China Pharmaceutical University
Pentacyclic triterpenes. Part 1: the first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases.
China Pharmaceutical University
Discovery of a potent and novel motilin agonist.
Bristol-Myers Squibb Pharmaceutical Research Institute
Studies on gambogic acid (IV): Exploring structure-activity relationship with I¿B kinase-beta (IKKß).
China Pharmaceutical University
Design and synthesis of novel photoaffinity probes for study of the target proteins of oleanolic acid.
China Pharmaceutical University
Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.
Amgen
Synthesis, biological evaluation and docking studies of octane-carboxamide based renin inhibitors with extended segments toward S3' site of renin.
China Pharmaceutical University
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.
Chinese Academy of Sciences
Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
University of Michigan
Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors.
China Pharmaceutical University
Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.
University of Toronto
Efficient synthesis and biological evaluation of epiceanothic acid and related compounds.
China Pharmaceutical University
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
University of Michigan
Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase.
China Pharmaceutical University
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
Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonists
TBA
Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
Chinese Academy of Sciences
Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspases.
University of Michigan
Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.
Amgen
Inhibition of Son of Sevenless Homologue 1 (SOS1): Promising therapeutic treatment for KRAS-mutant cancers.
China Pharmaceutical University
NRF2 inhibitors: Recent progress, future design and therapeutic potential.
Nanjing University of Chinese Medicine
Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma.
Chinese Academy of Sciences
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads.
Shaoxing University
Current therapy in amyotrophic lateral sclerosis (ALS): A review on past and future therapeutic strategies.
Nanjing University of Chinese Medicine
Discovery of Dehydrogenated Imipridone Derivatives as Activators of Human Caseinolytic Protease P.
China Pharmaceutical University
New insights into butyrylcholinesterase: Pharmaceutical applications, selective inhibitors and multitarget-directed ligands.
China Pharmaceutical University
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
Arvinas LLC
Discovery of Novel PD-L1 Small-Molecular Inhibitors with Potent In Vivo Anti-tumor Immune Activity.
China Pharmaceutical University
Design, Synthesis, and Antitumor Activity Evaluation of Novel VISTA Small Molecule Inhibitors.
China Pharmaceutical University
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model.
Sorbonne Universit£
Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application.
China Pharmaceutical University
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.
BeiGene(Beiing) Co., Ltd.
Butyrylcholinesterase-Activated Near-Infrared Fluorogenic Probe for In Vivo Theranostics of Alzheimer's Disease.
China Pharmaceutical University
Optimizing drug-like properties of selective butyrylcholinesterase inhibitors for cognitive improvement: Enhancing aqueous solubility by disrupting molecular plane.
China Pharmaceutical University
Discovery of 4-benzylpiperazinequinoline BChE inhibitor that suppresses neuroinflammation for the treatment of Alzheimer's disease.
China Pharmaceutical University
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis.
China Pharmaceutical University
Identification of a Novel, Potent, and Orally Bioavailable Guanidine-Based SHP2 Allosteric Inhibitor from Virtual Screening and Rational Structural Optimization for the Treatment of KRAS Mutant Cancers.
China Pharmaceutical University
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.
Shanghai Institute of Materia Medica
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Amgen
Development of highly potent and specific AKR1C3 inhibitors to restore the chemosensitivity of drug-resistant breast cancer.
China Pharmaceutical University
Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease.
China Pharmaceutical University
A highly effective and stable butyrylcholinesterase inhibitor with multi-faceted neuroprotection and cognition improvement.
Qingdao University
Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.
China Pharmaceutical University
Therapeutic potential of targeting kynurenine pathway in neurodegenerative diseases.
Shaoxing University
Discovery of the First Subnanomolar PPARα/δ Dual Agonist for the Treatment of Cholestatic Liver Diseases.
China Pharmaceutical University
Discovery of Potent and Wild-Type-Sparing Fourth-Generation EGFR Inhibitors for Treatment of Osimertinib-Resistance NSCLC.
China Pharmaceutical University
Structure-activity relationship study of amidobenzimidazole derivatives as stimulator of interferon genes (STING) agonists.
Peking Union Medical College
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Merck Research Laboratories
The Development and Design Strategy of Leucine-Rich Repeat Kinase 2 Inhibitors: Promising Therapeutic Agents for Parkinson's Disease.
China Pharmaceutical University
Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.
Beigene (Beijing) Co.
Design and Synthesis of Sulfonium Derivatives: A Novel Class of α-Glucosidase Inhibitors with Potent In Vivo Antihyperglycemic Activities.
China Pharmaceutical University
Design, synthesis and evaluation of fused hybrids with acetylcholinesterase inhibiting and Nrf2 activating functions for Alzheimer's disease.
China Pharmaceutical University
Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.
China Pharmaceutical University
Therapeutic potential of targeting SHP2 in human developmental disorders and cancers.
Zhejiang University
Strategies for Structural Modification of Small Molecules to Improve Blood-Brain Barrier Penetration: A Recent Perspective.
China Pharmaceutical University
Recent research progress of Uncaria spp. based on alkaloids: phytochemistry, pharmacology and structural chemistry.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein-Protein Interactions between DOT1L and MLL-AF9/MLL-ENL.
China Pharmaceutical University
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020).
Nanjing University of Chinese Medicine
The Design and Optimization of Monomeric Multitarget Peptides for the Treatment of Multifactorial Diseases.
China Pharmaceutical University
-Benzyl Benzamide Derivatives as Selective Sub-Nanomolar Butyrylcholinesterase Inhibitors for Possible Treatment in Advanced Alzheimer's Disease.
China Pharmaceutical University
Is a Highly Selective and Potent κ Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity.
Fudan University
Pentacyclic triterpenes. Part 2: Synthesis and biological evaluation of maslinic acid derivatives as glycogen phosphorylase inhibitors.
China Pharmaceutical University
The structure-based design of peptidomimetic inhibitors against SARS-CoV-2 3C like protease as Potent anti-viral drug candidate.
Nankai University
Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.
Shaoxing University
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.
Chinese Academy of Sciences
Discovery of Novel Aldo-Keto Reductase 1C3 Inhibitors as Chemotherapeutic Potentiators for Cancer Drug Resistance.
China Pharmaceutical University
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
Shaoxing University
Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors.
Jinan University
Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
Ludwig-Maximilians University
Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands.
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie
Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.
Peking Union Medical College
STING, a promising target for small molecular immune modulator: A review.
China Pharmaceutical University
Novel Electrophilic Warhead Targeting a Triple-Negative Breast Cancer Driver in Live Cells Revealed by "Inverse Drug Discovery".
Jinan University
Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis.
China Pharmaceutical University
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.
Chinese Academy of Sciences
Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection.
China Pharmaceutical University
First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate.
Takeda California
Syntheses, Biological Evaluations, and Mechanistic Studies of Benzo[
China Pharmaceutical University
Noncovalent EGFR T790M/L858R inhibitors based on diphenylpyrimidine scaffold: Design, synthesis, and bioactivity evaluation for the treatment of NSCLC.
Dalian Medical University
Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in the brain without affecting that in intestine.
China Pharmaceutical University
Synthesis and biological evaluation of selenogefitinib for reducing bleomycin-induced pulmonary fibrosis.
Dalian Medical University
Discovery of chiral N-2'-aryletheryl-1'-alkoxy-ethyl substituted arylisoquinolones with anti-inflammatory activity from the nucleophilic addition reactions of the thiophenols and oxazolinium.
Chinese Academy of Sciences
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).
China Pharmaceutical University
The components and activities analysis of a novel anticoagulant candidate dHG-5.
University of Chinese Academy of Sciences
Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb Research and Development
Bicyclic Ligand-Biased Agonists of S1P
Bristol Myers Squibb Research & Early Development
Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions.
City University of Hong Kong
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.
China Pharmaceutical University
Novel BuChE-IDO1 inhibitors from sertaconazole: Virtual screening, chemical optimization and molecular modeling studies.
Southwest University
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Beijing Normal University
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
China Pharmaceutical University
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists.
Bristol Myers Squibb
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
China Pharmaceutical University
N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies.
China Pharmaceutical University
Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.
Sun Yat-Sen University
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.
China Pharmaceutical University
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.
Bristol Myers Squibb
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
Jiangsu Aosaikang Pharmaceutical
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor.
China Pharmaceutical University
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.
China Pharmaceutical University
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.
Dalian Medical University
Peptide-based and small synthetic molecule inhibitors on PD-1/PD-L1 pathway: A new choice for immunotherapy?
China Pharmaceutical University
Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification.
China Pharmaceutical University
Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.
Jinan University
Advances in inhibition of protein-protein interactions targeting hypoxia-inducible factor-1 for cancer therapy.
China Pharmaceutical University
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.
Jiangsu Aosaikang Pharmaceutical
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.
East China Normal University
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
TBA
CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
Shaoxing University
Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
China Pharmaceutical University
Reasonably activating Nrf2: A long-term, effective and controllable strategy for neurodegenerative diseases.
China Pharmaceutical University
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.
National Institute of Biological Sciences (Nibs)
Molecular modeling and synthesis of inhibitors of herpes simplex virus type 1 uracil-DNA glycosylase.
University of Massachusetts Medical Center
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
TBA
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Glaxosmithkline
Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation.
Shaoxing University
Small molecule modulators targeting protein kinase CK1 and CK2.
China Pharmaceutical University
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
China Pharmaceutical University
Discovery of a Highly Selective and Potent κ Opioid Receptor Agonist from
Fudan University
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
China Pharmaceutical University
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.
China Pharmaceutical University
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.
National Center For Advancing Translational Sciences
Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin.
China Pharmaceutical University
Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors.
China Pharmaceutical University
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
China Pharmaceutical University
Identification of potent Yes1 kinase inhibitors using a library screening approach.
Frederick National Laboratory For Cancer Research
Discovery of natural estrogen receptor modulators with structure-based virtual screening.
East China University of Science and Technology
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.
Xi'An Jiaotong University
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.
Pfizer
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC).
Dalian Medical University
Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.
China Pharmaceutical University
Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines.
Dalian Medical University
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.
China Pharmaceutical University
Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease.
China Pharmaceutical University
Peptidomimetics for Targeting Protein-Protein Interactions between DOT1L and MLL Oncofusion Proteins AF9 and ENL.
China Pharmaceutical University
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
Cyclic Peptidic Mimetics of Apollo Peptides Targeting Telomeric Repeat Binding Factor 2 (TRF2) and Apollo Interaction.
China Pharmaceutical University
Design, synthesis and biological evaluation of 4,7,12,12a-tetrahydro-5H-thieno[3',2':3,4]pyrido[1,2-b]isoquinolines as novel adenosine 5'-monophosphate-activated protein kinase (AMPK) indirect activators for the treatment of type 2 diabetes.
Shanghai Institute of Materia Medica
Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
China Pharmaceutical University
Design, synthesis and evaluation of novel bivalent β-carboline derivatives as multifunctional agents for the treatment of Alzheimer's disease.
China Pharmaceutical University
Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib.
Fudan University
Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease.
China Pharmaceutical University
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na
Department of Discovery Chemistry Merck
ENPP1 Inhibitors and Methods of Modulating Immune Response
The Leland Stanford Junior University
SUBSTITUTED PHENYLPROPIONIC ACID DERIVATIVE AND USE THEREOF
Tuojie Biotech (Shanghai) Co.
NOVEL BENZOFURAN, BENZOTHIOPHENE, AND INDOLE ANALOGS THAT INHIBIT THE FORMATION OF TAU OLIGOMERS AND THEIR METHOD OF USE
Oligomerix
INHIBITORS OF THE INTERACTION BETWEEN TRIP8B AND HCN CHANNELS AND USES THEREOF FOR TREATING NEUROLOGICAL DISEASES AND DISORDERS
Northwestern University
Substituted pyrrolo[2,3-d]pyrimidines and pyrazolo[3,4-d]pyrimidines as inhibitors for multi-resistant cancers
Ferris State University
Structure-Guided Design of Conformationally Constrained Cyclohexane Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3CL Protease.
Wichita State University
Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
Incyte
Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors
Acetylon Pharmaceuticals
4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds as TAK1 inhibitors in disease treatment
Confluence Life Sciences
Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme.
Dumlupinar University
Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers.
Panjab University
Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli.
Astrazeneca India
17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
Universitaet Des Saarlandes
Desensitization of the human motilin receptor by motilides.
Katholieke Universiteit Leuven
Pharmacological profiles for rat cortical M1 and M2 muscarinic receptors using selective antagonists: comparison with N1E-115 muscarinic receptors.
Mayo Clinic
Novel small-molecule inhibitors of anthrax lethal factor identified by high-throughput screening.
Montana State University
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.
Merck Research Laboratories