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Article Title
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The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.

Amgen
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays.

College of Chemical and Environmental Engineering
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.

Sun Yat-Sen University
Synthesis, identification, and biological activity of metabolites of two novel selective S1P1 agonists.

Peking Union Medical College
Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors.

Chinese Academy of Sciences
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.

Bristol-Myers Squibb
Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.

Astrazeneca
Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.

Peking Union Medical College
Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening.

Chinese Academy of Sciences
Prediction of anti-tumor chemical probes of a traditional Chinese medicine formula by HPLC fingerprinting combined with molecular docking.

The Second People'S Hospital of Fujian Provinc
Thieno[3,2-b]thiophene-2-carboxylic acid derivatives as GPR35 agonists.

Corning
Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.

Eli Lilly
Design and synthesis of statine-containing BACE inhibitors.

Eli Lilly
Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists.

Corning
Evaluation of dihydropyrimidin-(2H)-one analogues and rhodanine derivatives as tyrosinase inhibitors.

Shaoyang University
Discovery and optimization of novel 3-piperazinylcoumarin antagonist of chemokine-like factor 1 with oral antiasthma activity in mice.

Peking Union Medical College
Design and synthesis of piperazine-indole p38alpha MAP kinase inhibitors with improved pharmacokinetic profiles.

Scios
Tetrahydro-β-carboline derivatives as potent histone deacetylase 6 inhibitors with broad-spectrum antiproliferative activity.

Northwest A&F University
Recent advances in the development of dual ALK/ROS1 inhibitors for non-small cell lung cancer therapy.

Weifang Medical University
Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease.

Northwest A&F University
Re-exploration of tetrahydro-β-carboline scaffold: Discovery of selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting and neuroprotective activities.

Yangling Vocational & Technical College
Discovery of 4-(Arylethynyl)piperidine Derivatives as Potent Nonsaccharide O-GlcNAcase Inhibitors for the Treatment of Alzheimer's Disease.

Chinese Academy of Medical Sciences and Peking Union Medical College
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia.

Chinese Academy of Medical Sciences & Peking Union Medical College
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.

Sichuan University
Discovery of a Promising CBP/p300 Degrader XYD129 for the Treatment of Acute Myeloid Leukemia.

Shenyang Pharmaceutical University
Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity.

Guangzhou Institutes of Biomedicine and Health
Design, Synthesis, and Antitumor Efficacy of Substituted 2-Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2.

Wuyi University
Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives.

Sichuan University
Precise Conformational Control Yielding Highly Potent and Exceptionally Selective BRD4 Degraders with Strong Antitumor Activity.

University of Michigan
Recent research advances in ATX inhibitors: An overview of primary literature.

Weifang Medical University
Structure-based design and synthesis of 2,4-diaminopyrimidines as EGFR L858R/T790M selective inhibitors for NSCLC.

Nanjing University of Science and Technology
Antitumor activity and structure-activity relationship of heparanase inhibitors: Recent advances.

Guangzhou University of Chinese Medicine
Reactive Oxygen Species (ROS)-Responsive Prodrugs, Probes, and Theranostic Prodrugs: Applications in the ROS-Related Diseases.

China Pharmaceutical University
Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors.

Guangzhou Medical University
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
Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer.

Guangzhou Medical University
Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.

East China Normal University
Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.

Chinese Academy of Sciences
Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.

Peking Union Medical College
Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors.

Weifang Medical University
Proteome-wide Identification of Off-Targets of a Potent EGFR

University of Macau
Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy.

Peking Union Medical College
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.

Jiangsu Ocean University
Discovery of

Peking Union Medical College
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2.

Second Military Medical University
Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders.

Icahn School of Medicine At Mount Sinai
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.

Maternal and Child Health Hospital of Hubei Province
Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide.

Henan University
Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation.

Hunan Agricultural University
S1P

Peking Union Medical College and Chinese Academy of Medical Sciences
Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors.

Sun Yat-Sen University
Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.

Sun Yat-Sen University
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.

University of Chinese Academy of Sciences
1-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.

Second Military Medical University
Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids.

Sun Yat-Sen University
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.

TBA
The discovery of a potent and selective third-generation EGFR kinase inhibitor as a therapy for EGFR L858R/T790M double mutant non-small cell lung cancer.

Sun Yat-Sen University
Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists.

Henan University
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.

Wuhan Polytechnic University
Development of Novel

East China University of Science and Technology
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.

Peking Union Medical College
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader.

Icahn School of Medicine At Mount Sinai
Homoisoflavonoids as potential imaging agents for β-amyloid plaques in Alzheimer's disease.

Hefei University of Technology
Design, synthesis, and biological evaluation of histone deacetylase inhibitors possessing glutathione peroxidase-like and antioxidant activities against Alzheimer's disease.

Sun Yat-Sen University
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
Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold.

Shenyang Pharmaceutical University
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.

University of Michigan Comprehensive Cancer Center
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.

Chinese Academy of Sciences
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.

Wuxi Apptec (Shanghai)
Original endomorphin-1 analogues exhibit good analgesic effects.

The First Hospital of Lanzhou University
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.

Chinese Academy of Sciences
Original endomorphin-1 analogues exhibit good analgesic effects with minimal implications for human sperm motility.

The Reproductive Medicine Special Hospital of The First Hospital of Lanzhou University
Design, synthesis, and evaluation of multitarget-directed ligands against Alzheimer's disease based on the fusion of donepezil and curcumin.

Sun Yat-Sen University
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.

Astrazeneca
BICYCLIC INDAZOLE GLUCOCORTICOID RECEPTOR ANTAGONISTS

Corcept Therapeutics
SULFONAMIDE DERIVATIVES AND THEIR USE AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS

Department Of Health
Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof

Pharmakea
Heterocyclic kinase inhibitors

Novartis
Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro.

Mayo Clinic