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Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.

Shandong University
Discovery of novel BRD4 inhibitors by high-throughput screening, crystallography, and cell-based assays.

Nanchang University
Development of the First Generation of Disulfide-Based Subtype-Selective and Potent Covalent Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors.

East China University of Science and Technology
Synthesis and biological evaluation of novel hydroxybenzaldehyde-based kojic acid analogues as inhibitors of mushroom tyrosinase.

Hunan University of Science and Technology
Discovery of novel DNA methyltransferase 3A inhibitors via structure-based virtual screening and biological assays.

University of Science and Technology of China
Design, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold.

Shenyang Pharmaceutical University
Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines.

Georgia State University
Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.

East China University of Science & Technology
Identification of novel EZH2 inhibitors through pharmacophore-based virtual screening and biological assays.

College of Chemical and Environmental Engineering
Design, synthesis and biological evaluation of N,N-3-phenyl-3-benzylaminopropanamide derivatives as novel cholesteryl ester transfer protein inhibitor.

Shenyang Pharmaceutical University
Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening.

Shanghai University
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.

Second Military Medical University
PTP1B inhibitors from stems of Angelica keiskei (Ashitaba).

Chinese Academy of Sciences
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.

Chinese Academy of Sciences
Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening.

Chinese Academy of Sciences
Discovery of two aminoglycoside antibiotics as inhibitors targeting the menin-mixed lineage leukaemia interface.

Fuzhou University
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.

Chinese Academy of Sciences
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.

Chinese Academy of Sciences
Anthraquinone Derivatives as Potent Inhibitors of c-Met Kinase and the Extracellular Signaling Pathway.

Soochow University
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.

Georgia State University
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.

Chinese Academy of Sciences
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.

Chinese Academy of Sciences
Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase.

Chinese Academy of Sciences
Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.

Chinese Academy of Sciences
Development of a First-in-Class DNMT1/HDAC Inhibitor with Improved Therapeutic Potential and Potentiated Antitumor Immunity.

Shandong University
Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment.

Central South University
Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells.

Shanghai Jiao Tong University
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.

Zhejiang Sci-Tech University
Structure-Based Design and Discovery of a Potent and Cell-Active LC3A/B Covalent Inhibitor.

Fudan University
Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy.

Nanjing University of Chinese Medicine
Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader.

Shanghai Institute of Materia Medica
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists.

Fudan University
Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury.

Fudan University
Optimization of carbazole carboxamide RORγt agonists: Challenges in improving the metabolic stability and maintaining the agonistic activity.

Fudan University
Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC.

Nanchang University
An ATG4B inhibitor blocks autophagy and sensitizes Sorafenib inhibition activities in HCC tumor cells.

Yantai University
Chemical probe of AHL modulators on quorum sensing in Gram-Negative Bacteria and as antiproliferative agents: A review.

Zhengzhou University
Diarylacetylene piperidinyl amides as novel anxiolytics.

Johnson & Johnson Pharmaceutical Research and Development
Spiroarborin, an

Yunnan University
(-)-Epigallocatechin Gallate is a Noncompetitive Inhibitor of NAD Kinase.

Hangzhou Institute For Advanced Study
The discovery of a non-competitive GOT1 inhibitor, hydralazine hydrochloride, via a coupling reaction-based high-throughput screening assay.

Nanjing University of Chinese Medicine
Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-

Shanghai Institute of Materia Medica
Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction.

Nanjing University of Chinese Medicine
Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1).

Chinese Academy of Sciences
Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer.

China Pharmaceutical University
Dynamics of Post-Translational Modification Inspires Drug Design in the Kinase Family.

Soochow University
Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.

Fujian Medical University
Discovery of novel reversible monoacylglycerol lipase inhibitors via docking-based virtual screening.

Nanchang University
Discovery and characterization of a novel glucose-6-phosphate dehydrogenase (G6PD) inhibitor via high-throughput screening.

Nanjing University of Chinese Medicine
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.

Shanghaitech University
Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors.

Key Laboratory of Molecule Synthesis and Function Discovery (Fujian Province University)
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.

Chinese Academy of Sciences
Discovery of a novel 53BP1 inhibitor through AlphaScreen-based high-throughput screening.

Yantai University
Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.

Sun Yat-Sen University
Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity.

The R. W. Johnson Pharmaceutical Research Institute
Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor.

The R. W. Johnson Pharmaceutical Research Institute
Lead discovery, chemical optimization, and biological evaluation studies of novel histone methyltransferase SET7 small-molecule inhibitors.

University of Chinese Academy of Sciences
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.

China Pharmaceutical University
Licochalcone A suppresses the proliferation of sarcoma HT-1080 cells, as a selective R132C mutant IDH1 inhibitor.

Guizhou Medcial University
Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.

Shanghai Institute of Materia Medica
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation.

Shanghai Institute of Materia Medica
Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer.

Chinese Academy of Sciences
Discovery of a Potent and Selective NF-κB-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo.

Chinese Academy of Sciences
Discovery of 8-Methyl-pyrrolo[1,2-

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

Second Military Medical University
Discovery of DC_H31 as potential mutant IDH1 inhibitor through NADPH-based high throughput screening.

Huazhong Agricultural University
Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors.

Shanghai Institute of Materia Medica
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.

University of Chinese Academy of Sciences
Development and Characterization of a Fluorescent Probe for GLS1 and the Application for High-Throughput Screening of Allosteric Inhibitors.

China Pharmaceutical University
The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening.

Zhejiang Sci-Tech University
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.

Chinese Academy of Sciences
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors.

Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria.

Chinese Academy of Sciences
Discovery of Novel Disruptor of Silencing Telomeric 1-Like (DOT1L) Inhibitors using a Target-Specific Scoring Function for the (S)-Adenosyl-l-methionine (SAM)-Dependent Methyltransferase Family.

Chinese Academy of Sciences
Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.

Central South University
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.

Chinese Academy of Sciences
Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening.

Chinese Academy of Sciences
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.

Chinese Academy of Sciences
Discovery of potent DOT1L inhibitors by AlphaLISA based High Throughput Screening assay.

University of Science and Technology of China
Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.

Hebei University
Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening.

Shanghai University
Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations.

University of Jinan
Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation.

Zhejiang Sci-Tech University
Amide substituted indole compounds useful as TLR inhibitors

Bristol-Myers Squibb
LSD1 inhibitors and medical uses thereof

Constellation Pharmaceuticals
Pyrimidine derivative, method for preparing same and use thereof in medicine

TBA
Substituted oxopyridine derivatives

Bayer Pharma Aktiengesellschaft
Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea.

Kitasato University
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.

Eli Lilly
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.

Upjohn