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Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
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
A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR

Guangzhou Institutes of Biomedicine and Health
Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).

Green Valley Research Institute
Design and synthesis of substituted pyrido[3,2-d]-1,2,3-triazines as potential Pim-1 inhibitors.

Shenyang Pharmaceutical University
Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors.

Chinese Academy of Sciences
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.

Sichuan University
Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists.

Korea Institute of Science and Technology
Multifunctional coumarin derivatives: monoamine oxidase B (MAO-B) inhibition, anti-ß-amyloid (Aß) aggregation and metal chelation properties against Alzheimer's disease.

China Pharmaceutical University
Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.

Sun Yat-Sen University
Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90.

Chinese Academy of Sciences
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors.

Chinese Academy of Sciences
Thiophene-core estrogen receptor ligands having superagonist activity.

Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University)
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.

Sun Yat-Sen University
2-(4-Chlorophenyl)-2-oxoethyl 4-benzamidobenzoate derivatives, a novel class of SENP1 inhibitors: Virtual screening, synthesis and biological evaluation.

Shanghai Jiao Tong University
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.

Chinese Academy of Sciences
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.

Amgen
3D-QSAR studies on 4-hydroxyphenylpyruvate dioxygenase inhibitors by comparative molecular field analysis (CoMFA).

Zhejiang University
Pyrrolo[2,3-c]azepine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.

Sun Yat-Sen University
Isoform-selective inhibition of chrysin towards human cytochrome P450 1A2. Kinetics analysis, molecular docking, and molecular dynamics simulations.

Sun Yat-Sen University
Aryl sulfones as novel bradykinin B1 receptor antagonists for treatment of chronic pain.

Amgen
Exploring Degradation of Intrinsically Disordered Protein Yes-Associated Protein Induced by Proteolysis TArgeting Chimeras.

University of Florida
Discovery of Novel Mcl-1 Inhibitors with a 3-Substituted-1H-indole-1-yl Moiety Binding to the P1-P3 Pockets to Induce Apoptosis in Acute Myeloid Leukemia Cells.

Shenyang Pharmaceutical University
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis.

University of Kansas
Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of 4-(indolin-1-yl)-6-substituted-pyrido[3,2-d]pyrimidine derivatives as Mnk1/2 inhibitors.

Shenyang Pharmaceutical University
Structural Dynamics-Driven Discovery of Anticancer and Antimetastatic Effects of Diltiazem and Glibenclamide Targeting Urokinase Receptor.

Fuzhou University
Selective Covalent Targeting of Pyruvate Kinase M2 Using Arsenous Warheads.

Chinese Academy of Sciences
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
Discovery of Dual Function Agents That Exhibit Anticancer Activity via Catastrophic Nicotinamide Adenine Dinucleotide Depletion.

Nanchang University
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.

Amgen
Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties.

Shenyang Pharmaceutical University
Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7.

Shanghaitech University
Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy.

Innovation Research Institute of Traditional Chinese Medicine
Discovery of Highly Potent Nicotinamide Phosphoribosyltransferase Degraders for Efficient Treatment of Ovarian Cancer.

Second Military Medical University
Making Protein Degradation Visible: Discovery of Theranostic PROTACs for Detecting and Degrading NAMPT.

Second Military Medical University (Navy Medical University)
Identification of Antithrombotic Natural Products Targeting the Major Substrate Binding Pocket of Protein Disulfide Isomerase.

Fuzhou University
Metalloform-selective inhibition: synthesis and structure-activity analysis of Mn(II)-form-selective inhibitors of Escherichia coli methionine aminopeptidase.

Graduate School of Chinese Academy of Sciences
Discovery of Novel Imidazo[4,5-

Chinese Academy of Sciences
Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.

Shenyang Pharmaceutical University
Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.

Second Military Medical University
Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA).

University of Wollongong
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders.

Chinese Academy of Sciences
Discovery of Novel Pyrrolo[2,3-

Chinese Academy of Sciences
Proteome-wide Identification of Off-Targets of a Potent EGFR

University of Macau
Synergetic inhibition of genistein and D-glucose on alpha-glucosidase.

Sun Yat-Sen (Zhongshan) University
Optimization of 4,6-Disubstituted Pyrido[3,2-

Shenyang Pharmaceutical University
Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents.

Southeast University
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.

Guangzhou Institutes of Biomedicine and Health
Using porphyrins as albumin-binding molecules to enhance antitumor efficacies and reduce systemic toxicities of antimicrobial peptides.

Fuzhou University
Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors.

Fudan University
Design, synthesis and biological evaluation of dual Bcl-2/Mcl-1 inhibitors bearing 2-(1H-indol-4-yl)benzoic acid scaffold.

Shenyang Pharmaceutical University
Dihydro-β-agarofuran-Type Sesquiterpenoids from the Seeds of

Chinese Academy of Sciences
Screening and biological evaluation of a novel STAT3 signaling pathway inhibitor against cancer.

Dalian Medical University
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.

Jinan University
Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.

China Pharmaceutical University
A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.

Shenyang Pharmaceutical University
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.

Chinese Academy of Sciences
Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction.

Chinese Academy of Sciences
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.

University of Wollongong
Histone acetyltransferase inhibitors: An overview in synthesis, structure-activity relationship and molecular mechanism.

Sichuan University
Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.

Southeast University
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.

Shandong University
Design and Optimization of 3'-(Imidazo[1,2-

Jinan University
Discovery and structure-activity-relationship study of novel imidazole cyclopropyl amine analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.

Shanghai Haihe Pharmaceutical
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.

Aarhus University
Identification of a New RXRα Antagonist Targeting the Coregulator-Binding Site.

Xiamen University
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.

Kyung Hee University
Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives.

Peking Union Medical College
Design, synthesis and biological evaluation of ring A modified 11-keto-boswellic acid derivatives as Pin1 inhibitors with remarkable anti-prostate cancer activity.

Shenyang Pharmaceutical University
Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design.

Shenyang Pharmaceutical University
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-Raf

Yantai University
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.

University of Wollongong
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.

Shanghai Haihe Pharmaceutical
Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.

Shanghai Haihe
Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.

Shanghai Haihe Pharmaceutial
Conjugates of 18β-glycyrrhetinic acid derivatives with 3-(1H-benzo[d]imidazol-2-yl)propanoic acid as Pin1 inhibitors displaying anti-prostate cancer ability.

Shenyang Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.

Chinese Academy of Sciences
TRICYCLIC COMPOUND AND USE THEREOF

Nanjing Zaiming Pharmaceutical
Annulated glycosidase inhibitors

Asceneuron
Pyridyl substituted indole compounds

Bristol-Myers Squibb
Dopamine D3 receptor antagonists having a morpholine moiety

Indivior
Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds

Array Biopharma
Aniline derivatives, their preparation and their therapeutic application

Fovea Pharmaceuticals
Purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient

Medpacto
Screening and X-ray crystal structure-based optimization of autotaxin (ENPP2) inhibitors, using a newly developed fluorescence probe.

The University of Tokyo
Bicyclic heterocycles as FGFR inhibitors

Incyte Holdings