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Article Title
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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
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.

Janssen Research and Development
Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).

Johnson & Johnson Pharmaceutical Research & Development
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.

Chinese Academy of Sciences
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.

Chinese Academy of Sciences
Discovery of 2,4,6-trisubstituted pyrimidine derivatives as novel potent HIV-1 NNRTIs by exploiting the tolerant region II of the NNIBP.

Shandong University
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
Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis.

Guangzhou Medical University
Structure-Based Drug Design of 2-Amino-[1,1'-biphenyl]-3-carboxamide Derivatives as Selective PKMYT1 Inhibitors for the Treatment of CCNE1-Amplified Breast Cancer.

Jinan University
Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3'-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury.

Shanghai Jiao Tong University
Discovery of Novel Aryl Triazolone Dihydropyridines (ATDPs) Targeting Highly Conserved Residue W229 as Promising HIV-1 NNRTIs.

Shandong University
Development of Antibacterial Peptides with Membrane Disruption and Folate Pathway Inhibitory Activities against Methicillin-Resistant Staphylococcus aureus.

Qilu University of Technology (Shandong Academy of Sciences)
Structure-Based Design and Discovery of a Potent and Cell-Active LC3A/B Covalent Inhibitor.

Fudan University
Pyrrole-containing hybrids as potential anticancer agents: An insight into current developments and structure-activity relationships.

Jiangxi Science & Technology Normal University
Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor.

Nanjing University of Chinese Medicine
LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake.

New York University School of Medicine
Recent advances in gout drugs.

Peking University
Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.

Sichuan University
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery.

Sichuan University
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.

Guangdong Pharmaceutical University
Disubstituted pyrimidine-5-carboxamide derivatives as novel HIV-1 NNRTIs: Crystallographic overlay-based molecular design, synthesis, and biological evaluation.

Shandong University
In situ click chemistry-based discovery of 1,2,3-triazole-derived diarylpyrimidines as novel HIV-1 NNRTIs by exploiting the tolerant region I in binding pocket.

Shandong University
Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection.

China Innovation Center of Roche
Discovery of a Potent, Cooperative, and Selective SOS1 PROTAC ZZ151 with In Vivo Antitumor Efficacy in KRAS-Mutant Cancers.

Shanghai Institute of Materia Medica
Synthesis and antineoplastic activity of ethylene glycol phenyl aminoethyl ether derivatives as FOXM1 inhibitors.

Peking Union Medical College
Lead Optimization and Avoidance of Metabolic-perturbing Motif Developing Novel Diarylpyrimidines as Potent HIV-1 NNRTIs.

Shandong University
Hypouricemic Actions of the Pericarp of Mangosteen

Kunming Medical University
Design, Synthesis, and Bioevaluation of Pyrido[2,3-

Nanjing University of Chinese Medicine
The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.

Jiangxi Science & Technology Normal University
Chemical synthesis and pharmacological properties of heparin pentasaccharide analogues.

Chinese Academy of Sciences
Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.

Shanghai Institute of Materia Medica
Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.

Guangdong Pharmaceutical University
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.

Guangdong Pharmaceutical University
Stapled peptides as scaffolds for developing radiotracers for intracellular targets: Preliminary evaluation of a radioiodinated MDM2-binding stapled peptide in the SJSA-1 osteosarcoma model.

Duke University Medical Center
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.

Chinese Academy of Sciences
Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor.

Zhejiang University
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.

Chinese Academy of Sciences
Design of Dimeric Bile Acid Derivatives as Potent and Selective Human NTCP Inhibitors.

National Institute of Biological Sciences
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.

Guangdong Pharmaceutical University
Design, synthesis, and biological studies of novel 3-benzamidobenzoic acid derivatives as farnesoid X receptor partial agonist.

Guangdong Pharmaceutical University
Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of

Chinese Academy of Sciences
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.

Shandong University
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.

Jiangxi Science & Technology Normal University
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.

Jiangxi Science & Technology Normal University
Lycosquarrines A-R,

China Pharmaceutical University
Design and synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors.

3-Dimensional Pharmaceuticals
Engineering of a Potent, Long-Acting NPY2R Agonist for Combination with a GLP-1R Agonist as a Multi-Hormonal Treatment for Obesity.

The Scripps Research Institute
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.

3-Dimensional Pharmaceuticals
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.

3-Dimensional Pharmaceuticals
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.

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

Roche Innovation Center Shanghai
Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.

Guangdong Pharmaceutical University
A New Approach of Mitigating CYP3A4 Induction Led to the Discovery of Potent Hepatitis B Virus (HBV) Capsid Inhibitor with Optimal ADMET Profiles.

TBA
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.

Calibr At The Scripps Research Institute
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.

Shandong University
Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.

Roche Innovation Center Shanghai
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.

Shandong University
Design and synthesis of 3,5-diaryl-4,5-dihydro-1H-pyrazoles as new tyrosinase inhibitors.

Sun Yat-Sen University
Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.

Guangdong Pharmaceutical University
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.

Shandong University
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.

Shandong University
Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives.

Luoyang Normal University
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.

Shandong University
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.

Soochow University
Design, synthesis, and discovery of 5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones and related derivatives as novel inhibitors of mPGES-1.

University of Kentucky
Discovery of Thiophene[3,2-

Shandong University
Selective inhibitors of human mPGES-1 from structure-based computational screening.

University of Kentucky
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Shandong University
Discovery of potent and selective CDK8 inhibitors through FBDD approach.

Roche Innovation Center Shanghai
New potent and selectiveαvβ

Jiangnan University
INHIBITORS OF RNA HELICASE DHX9 AND USES THEREOF

Accent Therapeutics
Kinase inhibitors

Topivert Pharma
Cycloalkylamines as monoamine reuptake inhibitors

Sunovion Pharamceuticals
2,5-disubstituted thiomorpholine orexin receptor antagonists

Merck Sharp & Dohme
Development of bombesin analogs with conformationally restricted amino acid substitutions with enhanced selectivity for the orphan receptor human bombesin receptor subtype 3.

National Institutes of Health
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Merck Research Laboratories