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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
Monascustin, an Unusual¿-Lactam from Red Yeast Rice.

Beijing Union University
Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors.

Shandong University
Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.

Shandong University
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.

Second Military Medical University
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.

Infinity Pharmaceuticals
Development of hydroxy-based sphingosine kinase inhibitors and anti-inflammation in dextran sodium sulfate induced colitis in mice.

Peking Union Medical College
Structure-based optimization of a peptidyl inhibitor against calcineurin-nuclear factor of activated T cell (NFAT) interaction.

The Ohio State University
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.

The Hong Kong Polytechnic University
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.

Shandong University
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.

Shandong University
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.

Shandong University
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.

Zhejiang University
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.

Zhejiang University
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.

Zhejiang University
Discovery of small molecular inhibitors targeting HIV-1 gp120-CD4 interaction drived from BMS-378806.

Shandong University
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.

Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed fromß-amino acid as proteasome inhibitors.

Zhejiang University
Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.

Zhejiang University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.

Zhejiang University
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.

Zhejiang University
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.

Zhejiang University
Amide-based derivatives ofß-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects.

University of Sydney
Synthetic silvestrol analogues as potent and selective protein synthesis inhibitors.

Infinity Pharmaceuticals
Discovery of a novel series of inhibitors of lymphoid tyrosine phosphatase with activity in human T cells.

University of Southern California
Design, synthesis and biological activity of 6-substituted carbamoyl benzimidazoles as new nonpeptidic angiotensin II AT1 receptor antagonists.

School of Chemical Engineering & The Environment
Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents.

Sichuan University
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.

Zhejiang University
Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT1 receptor antagonists.

Beijing Institute of Technology
Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.

The Scripps Research Institute
Spacer length effects on in vitro imaging and surface accessibility of fluorescent inhibitors of prostate specific membrane antigen.

Washington State University
Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.

Zhejiang University
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.

Zhejiang University
A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.

Washington State University
Synthesis and biological activity of 5-[(2,5-dihydroxybenzyl)amino]salicylic acid analogs as inhibitors of EGF receptor-associated protein tyrosine kinase

TBA
Synthesis and screening of a cyclic peptide library: discovery of small-molecule ligands against human prolactin receptor.

The Ohio State University
Design, synthesis and biological evaluation of novel SIRT3 inhibitors targeting both NAD+ and substrate binding sites for the treatment of acute myeloid leukemia.

Shihezi University
Development of novel antivrial agents that induce the degradation of the main protease of human-infecting coronaviruses.

Chinese Academy of Sciences
Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors.

Shenyang Pharmaceutical University
Structure-based discovery of a new series of nucleoside-derived ring-opening PRMT5 inhibitors.

University of Chinese Academy of Sciences
Discovery of Tetrahydropyrazolopyrazine Derivatives as Potent and Selective MYT1 Inhibitors for the Treatment of Cancer.

Insilico Medicine Shanghai Ltd
Discovery of Novel HDAC3 Inhibitors with PD-L1 Downregulating/Degrading and Antitumor Immune Effects.

Southern Medical University
Glycan-Modified Peptides for Dual Inhibition of Human Immunodeficiency Virus Entry into Dendritic Cells and T Cells.

Chinese Academy of Sciences
Structure-Based Design and Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High Selectivity, Brain Penetration, and In Vivo Efficacy.

Suzhou Genhouse Bio
Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy.

Southern Medical University
Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors.

Central South University
Design, synthesis and biological evaluation of 2-aminopyrimidine derivatives as potent FLT3 inhibitors.

Zhejiang University
Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1.

Pfizer
SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: taming hERG.

Schering-Plough Research Institute
Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.

Zhejiang University
Reprogramming Energy Metabolism with Synthesized PDK Inhibitors Based on Dichloroacetate Derivatives and Targeted Delivery Systems for Enhanced Cancer Therapy.

Wuhan University
Discovery and Crystallography Study of Novel Biphenyl Ether and Oxadiazole Thioether (Non-Arylmethylamine)-Based Small-Molecule PD-1/PD-L1 Inhibitors as Immunotherapeutic Agents.

Southern Medical University
Design and synthesis of a potent histone deacetylase inhibitor.

Virginia Tech
X-ray Crystal Structure-Guided Discovery of Novel Indole Analogues as Colchicine-Binding Site Tubulin Inhibitors with Immune-Potentiating and Antitumor Effects against Melanoma.

Southern Medical University
Discovery of novel and selective SIK2 inhibitors by the application of AlphaFold structures and generative models.

Insilico Medicine Shanghai
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib.

Anhui University of Chinese Medicine
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.

Zhejiang University
Development of a series of quinazoline-2,5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.

Shanghai Institute of Materia Medica
Emerging targets and potential therapeutic agents in non-alcoholic fatty liver disease treatment.

Sichuan University
Discovery of pyrido[4,3-d]pyrimidinone derivatives as novel Wee1 inhibitors.

Zhejiang University
Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents.

Northwest A&F University
Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment.

Shandong First Medical University and Shandong Academy of Medical Sciences
Discovery of Novel

Shenyang Pharmaceutical University
Single and dual target inhibitors based on Bcl-2: Promising anti-tumor agents for cancer therapy.

Shandong First Medical University & Shandong Academy of Medical Sciences
p62 as a therapeutic target for tumor.

China Pharmaceutical University
PFKFB3 inhibitors as potential anticancer agents: Mechanisms of action, current developments, and structure-activity relationships.

Liaocheng University
Design, synthesis, and evaluation of pyrido.[3,4-b]pyrazin-2(1H)-one derivatives as potent FLT3 inhibitors.

Zhejiang University
Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-

Jinan University
Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy.

Southern Medical University
Efficient targeted oncogenic KRAS

Jinan University
Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.

Anhui Medical University
Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis.

Anhui Medical University
DYRK1A inhibitors for disease therapy: Current status and perspectives.

West China Hospital
The evolution paths of some reprehensive scaffolds of RORγt modulators, a perspective from medicinal chemistry.

Sun Yat-Sen University
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.

Shandong First Medical University & Shandong Academy of Medical Sciences
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.

Chinese Academy of Sciences
(-)-Epigallocatechin Gallate is a Noncompetitive Inhibitor of NAD Kinase.

Hangzhou Institute For Advanced Study
Recent progress in agents targeting polo-like kinases: Promising therapeutic strategies.

Shandong First Medical University & Shandong Academy of Medical Sciences
Cysteine derivatives as acetyl lysine mimics to inhibit zinc-dependent histone deacetylases for treating cancer.

Guizhou Medical University
Drug Repurposing of Quisinostat to Discover Novel

East China University of Science and Technology
Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT.

Zhejiang University
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.

University of Michigan
Indirubin Derivatives as Dual Inhibitors Targeting Cyclin-Dependent Kinase and Histone Deacetylase for Treating Cancer.

Guizhou Medical University
Discovery of Irbesartan Derivatives as BLT2 Agonists by Virtual Screening.

Fraunhofer Institute For Translational Medicine and Phamacology Itmp
Development of peptide epoxyketones as selective immunoproteasome inhibitors.

Zhejiang University
Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.

Zhejiang University
Design, synthesis, and biological evaluation of 2,4-diamino pyrimidine derivatives as potent FAK inhibitors with anti-cancer and anti-angiogenesis activities.

Guizhou Medical University
Discovery of novel CA-4 analogs as dual inhibitors of tubulin polymerization and PD-1/PD-L1 interaction for cancer treatment.

Southern Medical University
Synthesis and in vitro evaluation of novel spiroketopyrazoles as acetyl-CoA carboxylase inhibitors and potential antitumor agents.

Xuzhou Medical University
First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters.

Fraunhofer Ime
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.

Shandong First Medical University & Shandong Academy of Medical Sciences
Discovery of Novel

East China University of Science and Technology
Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3β inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents.

Anhui Medical University
Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions.

China Pharmaceutical University
Discovery of Novel and Highly Potent Resorcinol Dibenzyl Ether-Based PD-1/PD-L1 Inhibitors with Improved Drug-like and Pharmacokinetic Properties for Cancer Treatment.

Southern Medical University
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.

Shanghai Institute of Materia Medica
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.

Jinan University
Design, Synthesis, and Structure-Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.

China Pharmaceutical University
Galanthamine, Plicamine, and Secoplicamine Alkaloids from Zephyranthes candida and Their Anti-acetylcholinesterase and Anti-inflammatory Activities.

Huazhong University of Science and Technology
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.

East China Normal University
Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles.

Hangzhou Institute of Innovative Medicine
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.

Zhejiang University
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase.

Yunnan University
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.

Zhejiang University
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.

Zhejiang University
Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.

Liaoning Shihua University
TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.

East China Normal University
A Series of Compounds Bearing a Dipyrido-Pyrimidine Scaffold Acting as Novel Human and Insect Pest Chitinase Inhibitors.

Dalian University of Technology
Synthesis, pharmacological evaluation, and mechanistic study of adefovir mixed phosphonate derivatives bearing cholic acid and l-amino acid moieties for the treatment of HBV.

Guizhou Medical University
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.

Northwest University
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.

Zhejiang University
Nonpeptidic angiotensin II AT₁ receptor antagonists derived from 6-substituted aminocarbonyl and acylamino benzimidazoles.

Beijing Institute of Technology
Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.

Zhejiang University
Caffeic acid derivatives: a new type of influenza neuraminidase inhibitors.

Shandong University
Development of Unsymmetrical Dyads As Potent Noncarbohydrate-Based Inhibitors against Human β-N-Acetyl-d-hexosaminidase.

East China University of Science and Technology
Membrane permeable cyclic peptidyl inhibitors against human Peptidylprolyl Isomerase Pin1.

The Ohio State University
Discovery and development of substituted tyrosine derivatives as Bcl-2/Mcl-1 inhibitors.

Shandong University
Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids.

Peking Union Medical College
Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide.

China Pharmaceutical University
Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway.

China Pharmaceutical University
Discovery of a head-to-tail cyclic peptide as the Keap1-Nrf2 protein-protein interaction inhibitor with high cell potency.

China Pharmaceutical University
Preparation of 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives and their activity against DOT1L.

Shenyang Pharmaceutical University
1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation.

Shandong University
Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.

Shenyang Pharmaceutical University
Antimitotic amides for the treatment of cancer and proliferative disorders

Frost Biologic
HETEROCYCLIC COMPOUNDS AS UBIQUITIN SPECIFIC PROTEASE 7 INHIBITORS

Almac Discovery
SUBSTITUTED N-CYANOPYRROLIDINES WITH ACTIVITY AS USP30 INHIBITORS

Mission Therapeutics
TYRO3 INHIBITORS

Halia Therapeutics
Cycloalkane derivatives

Daiichi Sankyo
Methylene linked quinolinyl modulators of RORγt

Janssen Pharmaceutica
Chemotype-selective modes of action of ¿-opioid receptor agonists.

University of North Carolina