PMID
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Article Title
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Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome.

National Institute of Biological Sciences
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.

Wuhan University School of Pharmaceutical Sciences
Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the 'reversed' amide scaffold.

Soochow University
Discovery of Novel 15-Lipoxygenase Activators To Shift the Human Arachidonic Acid Metabolic Network toward Inflammation Resolution.

University of California San Diego
SAR exploration at the C-3 position of tetrahydro-ß-carboline sstr3 antagonists.

Merck Research Laboratories
Identification of benzothiophene amides as potent inhibitors of human nicotinamide phosphoribosyltransferase.

Second Military Medical University
Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors.

Soochow University
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.

Merck Research Laboratories
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.

Merck Research Laboratories
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.

Fujian University of Traditional Chinese Medicine
Investigation of Cardiovascular Effects of Tetrahydro-ß-carboline sstr3 antagonists.

Merck Research Laboratories
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.

Merck Research Laboratories
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1.

Peking University
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories
Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen.

Peking University
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.

TBA
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.

Peking University
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.

TBA
Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.

Merck Research Laboratories
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.

Merck Research Laboratories
Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.

Merck Research Laboratories
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.

Merck Research Laboratories
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.

Merck Research Laboratories
Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.

Amri
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.

Merck Research Laboratories
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

Merck Research Laboratories
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.

Merck Research Laboratories
Discovery of dual inhibitors targeting both HIV-1 capsid and human cyclophilin A to inhibit the assembly and uncoating of the viral capsid.

Peking University
Synthesis and evaluation of dihydrofuro[2,3-b]pyridine derivatives as potent IRAK4 inhibitors.

Soochow University
Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases.

Qingdao University
Smart glypican-3-targeting peptide-chlorin e6 conjugates for targeted photodynamic therapy of hepatocellular carcinoma.

Second Military Medical University (Naval Medical University)
Design, Synthesis, and Biological Evaluation of a Novel NIK Inhibitor with Anti-Inflammatory and Hepatoprotective Effects for Sepsis Treatment.

China Pharmaceutical University
Ligand- and structure-based identification of novel CDK9 inhibitors for the potential treatment of leukemia.

South China University of Technology
Development of highly potent and specific AKR1C3 inhibitors to restore the chemosensitivity of drug-resistant breast cancer.

China Pharmaceutical University
A highly effective and stable butyrylcholinesterase inhibitor with multi-faceted neuroprotection and cognition improvement.

Qingdao University
Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.

China Pharmaceutical University
Biological Function of Pin1 in Vivo and Its Inhibitors for Preclinical Study: Early Development, Current Strategies, and Future Directions.

Shanghai University
Discovery of AXL Degraders with Improved Potencies in Triple-Negative Breast Cancer (TNBC) Cells.

Jinan University
Discovery of Highly Potent Nicotinamide Phosphoribosyltransferase Degraders for Efficient Treatment of Ovarian Cancer.

Second Military Medical University
Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.

Second Military Medical University (Naval Medical University)
Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection.

Wuxi Apptec
Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors.

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

Second Military Medical University (Navy Medical University)
In silico, synthesis and anticancer evaluation of benzamide tryptamine derivatives as novel eEF2K inhibitors.

Ningbo University
The structure-based design of peptidomimetic inhibitors against SARS-CoV-2 3C like protease as Potent anti-viral drug candidate.

Nankai University
Discovery of Novel Aldo-Keto Reductase 1C3 Inhibitors as Chemotherapeutic Potentiators for Cancer Drug Resistance.

China Pharmaceutical University
Nucleic-Acid-Based Targeted Degradation in Drug Discovery.

Second Military Medical University
Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.

Jinan University
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity.

Soochow University
Hydrophobic Tagging-Induced Degradation of PDEδ in Colon Cancer Cells.

Second Military Medical University
Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection.

China Pharmaceutical University
Ring closure strategy leads to potent RIPK3 inhibitors.

Soochow University
Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity.

Soochow University
Structural optimization of aminopyrimidine-based CXCR4 antagonists.

Soochow University
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.

China Pharmaceutical University
Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B.

Merck
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor.

China Pharmaceutical University
Discovery of human lactate dehydrogenase 5 inhibitors (hLDH5) with anti-lung cancer activity through an in silico method and biological validation.

The 5Th Affiliated Hospital of Shenzhen University Health Science Center
Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ.

China Pharmaceutical University
Reasonably activating Nrf2: A long-term, effective and controllable strategy for neurodegenerative diseases.

China Pharmaceutical University
A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45.

Ningbo University
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.

Shaanxi University of Science & Technology
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Merck
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.

China Pharmaceutical University
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

Merck
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase.

Merck
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.

China Pharmaceutical University
High-affinity small-molecule inhibitors of the menin-mixed lineage leukemia (MLL) interaction closely mimic a natural protein-protein interaction.

University of Michigan
Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.

China Pharmaceutical University
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors.

East China University of Science and Technology
Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor.

Soochow University
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.

East China University of Science and Technology
Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.

Anhui Medical University
Design, Synthesis, and Evaluation of Tetrahydropyrrolo[1,2-

Wuxi Apptec (Shanghai)
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.

Merck
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.

East China University of Science & Technology
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.

National Institute of Diabetes and Digestive and Kidney Diseases
BICYCLIC TRIAZINE DERIVATIVES FOR THE TREATMENT OF CANCER

Deutsches Krebsforschungszentrum
COMPOUND SERVING AS NLRP3 INHIBITOR

Hangzhou Innogate Pharma
HETEROCYCLIC JAK INHIBITOR

Beijing Innocare Pharma Tech
Pyrimidinones as PI3K inhibitors

Incyte Holdings
Small molecule inhibitors of galectin-3

Bristol-Myers Squibb
Second generation GRP94-selective inhibitors

University of Kansas
Heteroaryl-substituted sulfonamide compounds and their use as therapeutic agents

Xenon Pharmaceuticals
Cyclohexene compounds and use thereof

Guangzhou Henovcom Bioscience
Purine inhibitors of human phosphatidylinositol 3-kinase delta

Merck Sharp & Dohme
Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.

Instituto Superior Técnico
Inhibitory effects of thioethers on fatty acid synthase and 3T3-L1 cells.

Graduate University of Chinese Academy of Sciences
Synthesis, structure-activity relationships studies of benzoxazinone derivatives as a-chymotrypsin inhibitors.

University of Karachi
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.

University of Manchester
Pyrimidine PDE10 inhibitors

Merck Sharp & Dohme
Spiroxazolidinone compounds

Merck Sharp & Dohme
Isoform-specific inhibition of cyclophilins.

Max Planck Research
Competitive inhibition of human poly(A)-specific ribonuclease (PARN) by synthetic fluoro-pyranosyl nucleosides.

University of Thessaly