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Identification of Direct-Acting nsP2 Helicase Inhibitors with Antialphaviral Activity.
J Med Chem 68: 14514-14536
University of North Carolina at Chapel Hill
Discovery of APH02174 as a Highly Selective and Orally Bioavailable IRAK4 Degrader for the Treatment of Inflammatory Diseases.
J Med Chem 68: 12845-12861
Sun Yat-sen University
Discovery and Crystallography Study of Novel Resorcinol Dibenzyl Ether-Based PD-1/PD-L1 Inhibitors with Improved Drug-like and Pharmacokinetic Properties for Cancer Treatment.
J Med Chem 68: 12593-12614
Southern Medical University
Discovery and Optimization of Potent PROTAC Degraders of Phosphoinositide 3-Kinase with Significant in Vivo Anticancer Efficacy.
J Med Chem 68: 12800-12818
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of a Selective, Novel TGF-βR1 Inhibitor GFH018 for the Treatment of Solid Tumors.
J Med Chem 68: 12513-12530
GenFleet Therapeutics (Zhejiang) Co. Ltd.
Prodrugs Targeting Prostate-Specific Membrane Antigen against Prostate Cancer.
J Med Chem 68: 12296-12330
National and Kapodistrian University of Athens (NKUA)
Could Hydrophobicity of Sulfated Pseudo-Trisaccharides Derived from Repurposing Aminoglycoside Tobramycin Modulate the Enzymatic Activity of Heparanase?
J Med Chem 68: 12708-12732
Wayne State University
Searching for Synthetic Opioid Rescue Agents. 2: Identification of an Ultra-Potent Synthetic Opioid Rescue Agent.
J Med Chem 68: 13057-13074
University of Kentucky
Discovery of BAY 3389934 Hydrochloride: A Potent and Selective Small-Molecule Dual Factor IIa/Xa Inhibitor with Short Half-Life for the Acute Treatment of Sepsis-Induced Coagulopathy.
J Med Chem 68: 12687-12707
Germany.F. Hoffmann-La Roche Ltd
Discovery of KDX1381, a Bivalent CK2α Inhibitor for the Treatment of Solid Tumors as a Single Agent or in Combination.
J Med Chem 68: 12819-12844
Kairos Discovery
Design and Synthesis of PARP/CDK6 Dual-Target Inhibitors Modulating of Wnt/β-Catenin Signaling Pathway for the Treatment of BRCA Wild-Type TNBC.
J Med Chem 68: 13030-13056
China Pharmaceutical University
Discovery of TBK1Molecular Glue Degraders as a Potential Strategy for the Treatment of Autosomal Dominant Polycystic Kidney Disease (ADPKD).
J Med Chem 68: 12862-12880
Jinan University
Validation, Key Pharmacophores, and X-ray Cocrystal Structures of Novel Biochemically and Cellularly Active WRN Inhibitors Derived from a DNA-Encoded Library Screen.
J Med Chem 68: 12434-12456
Abbvie
Heparan Sulfate-Based Neoproteoglycan for Targeted Lysosomal Degradation of Amyloid-β.
J Med Chem 68: 11979-11989
Indian Institute of Science Education and Research
Discovery of KIN-8741, a Highly Selective Type IIb c-Met Kinase Inhibitor with Broad Mutation Coverage and Quality Drug-Like Properties for the Treatment of Cancer.
J Med Chem 68: 10648-10662
Kinnate Biopharma Inc.
Optimization of 1-Methyl-3-(pyridin-3-yl)-1H-indol Derivatives as ROR1 Inhibitors with Improved Activity and Selectivity.
J Med Chem 68: 11188-11216
Sichuan University
Lysine-Targeted Covalent Strategy Leading to the Discovery of Novel Potent PROTAC-Based PI3Kδ Degraders.
J Med Chem 68: 11437-11467
Xi'an Jiaotong University
Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis.
J Med Chem 68: 10738-10756
University of South China
Harder than Metal: Challenging Antimicrobial Resistance with Metallo-β-lactamase Inhibitors.
J Med Chem 68: 10556-10576
University of Naples Federico II
Design of an Oral STING Agonist through Intramolecular Hydrogen Bond Ring Mimicking to Achieve Complete Tumor Regression.
J Med Chem 68: 11365-11385
University of Michigan
Structural Optimization of Next-Generation TRK Inhibitors against Acquired Drug Resistance Mutations for the Treatment of Solid Tumors.
J Med Chem 68: 11484-11501
Shanghai Institute of Materia Medica
The Discovery of C7-Substituted Norbornyl Bisamides as RXFP1 Small Molecule Agonists.
J Med Chem 68: 12185-12203
Bristol Myers Squibb, Co.
Design, Synthesis, and Biological Evaluation of New PDE4 Inhibitors for the Treatment of Pressure Ulcers.
J Med Chem 68: 11628-11647
Wuyi University
Discovery of AB801, a Potent and Selective Inhibitor of AXL Receptor Tyrosine Kinase for Use in Cancer Therapy.
J Med Chem 68: 10663-10676
Arcus Biosciences, Inc.
A "Ligand First" Approach toward Selective, Covalent JNK2/3 Inhibitors.
J Med Chem 68: 12004-12028
Eberhard Karls Universitat Tubingen
Discovery and Administration Optimization of Novel Selective CDK9 Inhibitor, 1-7a-B1, for Improved Pharmacokinetics and Antitumor Efficacy In Vivo.
J Med Chem 68: 11586-11605
Shenyang Pharmaceutical University
Structure-Based Design of Potent and Selective MerTK Inhibitors by Modulating the Conformation of αC Helix.
J Med Chem 68: 10877-10896
National Health Research Institutes
Discovery of a Potent FLT3 Inhibitor (E)-4-(3-(3-Fluoro-4-(morpholinomethyl)styryl)-1H-indazol-6-yl)pyridin-2-amine for the Treatment of Acute Myeloid Leukemia with Multiple FLT3 Mutations.
J Med Chem 68: 11894-11915
Sichuan University
Discovery of Highly Potent, Selective, and Liver-Targeting HSD17B13 Inhibitor with Robust In Vivo Anti-MASH Activity.
J Med Chem 68: 11127-11148
Guangdong Pharmaceutical University
Design of Potent Small-Molecule Stimulator of Interferon Gene Inhibitor and Stimulator of Interferon Gene Mutant-Specific Degrader.
J Med Chem 68: 11100-11126
University of Michigan
Development of Novel Phthalazinone-Triazole Hybrids as Potential Antidiabetic Agents Targeting GLUT4 Translocation in Skeletal Muscle.
J Med Chem 68: 10722-10737
CSIR-Central Drug Research Institute BS
Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor.
J Med Chem 68: 10631-10647
Repare Therapeutics, Inc.
Similar Binding Mode of a 5-Sulfonylthiouracil Derivative Antagonist at Chemerin Receptors CMKLR1 and GPR1.
J Med Chem 68: 11149-11173
Leipzig University
Medicinal Chemistry Progression of Sapanisertib, the Anticancer and Dual Plasmodium Phosphatidylinositol 4-Kinase Beta and cGMP-Dependent Protein Kinase Inhibitor, for Malaria.
J Med Chem 68: 10757-10770
University of Cape Town
Design, Synthesis, and Biological Evaluation of 4-(Difluoromethyl)-1H-imidazole-5-carboxylic Acids/4-(3-Cyanophenoxy)pyrimidine-5-carboxylic Acids as P2Y1 Receptor Antagonists for Ischemic Stroke Treatment.
J Med Chem 68: 10930-10952
Shenyang Pharmaceutical University
Diazepine Agonists of the 5-HT2C Receptor with Unprecedented Selectivity: Discovery of Bexicaserin (LP352).
J Med Chem 68: 10599-10618
Arena Pharmaceuticals
XPO1-Targeting Selective Inhibitors of Transcriptional Activation Suppress Graft-versus-Host Disease.
J Med Chem 68: 12141-12171
Case Western Reserve University
Novel Pyrido[3,4-d]pyrimidin-4-one and Pyrimido[5,4-d]pyrimidin-4-one Derivatives as TREM2 Agonists for Treating Parkinson's Disease.
ACS Med Chem Lett 16: 715-716
Smith, Gambrell & Russell
Targeting KRAS G12D Mutations: Advances in Small Molecule Inhibitors and PROTAC Technology.
ACS Med Chem Lett 16: 746-747
Usona Institute
Macrocyclization: Enhancing Drug-like Properties of Discoidin Domain Receptor Kinase Inhibitors.
ACS Med Chem Lett 16: 784-789
Chiesi Farmaceutici
Novel Compounds as NLRP3 Inhibitors for Treating Asthma or COPD.
ACS Med Chem Lett 16: 760-761
Smith, Gambrell & Russell
Novel 2-Pyrrolidone Derivatives as Negative Allosteric Modulators of GluN2B-Containing NMDA Receptors.
ACS Med Chem Lett 16: 719-720
Emory University
Novel Tricyclic Compounds as GSK3 Inhibitors.
ACS Med Chem Lett 16: 724-727
Emory University
Discovery of ONO-TR-772 (VU6018042): A Highly Selective and CNS Penetrant TREK Inhibitor in Vivo Tool Compound.
ACS Med Chem Lett 16: 896-901
Ono Pharmaceutical Co., Ltd
Novel Heterocyclic Pyrimidine Derivatives as GSK3α Inhibitors.
ACS Med Chem Lett 16: 721-723
Emory University
Novel Isoxazolidines Derivatives as RIPK1 Inhibitors for Treating Neurodegenerative Diseases.
ACS Med Chem Lett 16: 754-755
Smith, Gambrell & Russell
Discovery of Thieno[3,2-b]pyridine-5-carboxamide and 2,3-Difluorobenzamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5.
ACS Med Chem Lett 16: 865-874
Vanderbilt University
Novel Spirocyclic WRN Helicase Inhibitors for Treating Cancer.
ACS Med Chem Lett 16: 764-765
Smith, Gambrell & Russell LLP
IRAK1/4/pan-FLT3 Kinase Inhibitors with Reduced hERG Block as Treatments for Acute Myeloid Leukemia.
ACS Med Chem Lett 16: 887-895
National Center for Advancing Translational Sciences
Novel Substituted Cyclic Compounds as SLC6A19 Inhibitors for Treating Phenylketonuria and Other Amino Acidurias.
ACS Med Chem Lett 16: 734-735
Smith, Gambrell & Russell
Novel Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation.
ACS Med Chem Lett 16: 748-749
Emory University
Novel Azaindole Compounds as Phosphodiesterase 4B Inhibitors for Treating Immune-Inflammatory Diseases or Disorders.
ACS Med Chem Lett 16: 717-718
Emory University
Novel Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis.
ACS Med Chem Lett 16: 730-731
Smith, Gambrell & Russell
Novel Piperidine Substituted Pyrazolopyrimidine Derivatives as SGK1 Inhibitors for Treating Cardiovascular Diseases.
ACS Med Chem Lett 16: 762-763
Smith, Gambrell & Russell
Identification of a RANKL/TNF-α Dual-Inhibitor as a Potential Disease-Modifying Agent for the Treatment of Knee Osteoarthritis.
J Med Chem 68: 10216-10237
ShanghaiTech University
Discovery of a Chiral 2,4-Substituted Pyrrolo[2,3-d]pyrimidine as a Potent, Selective, and Orally Bioavailable LRRK2 Inhibitor.
J Med Chem 68: 9926-9946
Duke University School of Medicine
Discovery of 3-(Fluoro-imidazolyl)pyridazine Derivatives as Potent STING Agonists with Antitumor Activity.
J Med Chem 68: 9864-9885
Chinese Academy of Sciences
Rational Design of Dual Degraders by Incorporating Molecular Glue Structural Features into PROTAC Degraders.
J Med Chem 68: 10268-10298
Ocean University of China
Design, Synthesis, and Evaluation of Novel ROCK Inhibitors for Glaucoma Treatment: Insights into In Vitro and In Vivo Efficacy and Safety.
J Med Chem 68: 10008-10030
Shandong First Medical University & Shandong Academy of Medical Sciences
Discovery of Highly Potent and Selective EZH2 Covalent Inhibitors via Incorporating Basic Amines.
J Med Chem 68: 10365-10383
Sun Yat-Sen University
Discovery and Characterization of RP03707: A Highly Potent and Selective KRASG12D PROTAC.
J Med Chem 68: 10238-10254
Risen (Shanghai) Pharma Tech Co., Ltd.
De Novo 3-(Phenylcarbamoyl) Benzoate Analogues: Efficacy against Multidrug-Resistant S. aureus and Elucidation of the Biodistribution Profile.
J Med Chem 68: 10329-10345
Indian Institute of Technology Kanpur
A First-in-Class Hepatocyte Nuclear Factor 4 Agonist.
J Med Chem 68: 10410-10424
Goethe University Frankfurt
Discovery of P11-2: A Potent First-in-Class MNK1-Targeting PROTAC Degrader for the Treatment of Cancer.
J Med Chem 68: 10092-10110
Guangdong Pharmaceutical University
New Insights into the French Paradox: Free Radical Scavenging by Resveratrol Yields Cardiovascular Protective Metabolites.
J Med Chem 68: 10031-10047
University of Szeged
Structure-Guided Optimization of 2-Aminoquinazoline Hematopoietic Progenitor Kinase 1 Inhibitors for Improved Oral Bioavailability and Synergistic Antitumor Immunity.
J Med Chem 68: 10439-10460
China Pharmaceutical University
A Perspective on the Strategic Application of Deconstruction-Reconstruction in Drug Discovery.
J Med Chem 68: 10520-10539
AstraZeneca
Design, Synthesis, and Biological Evaluation of Novel Activators of Human Caseinolytic Protease P with a Pyrazololactam Scaffold.
J Med Chem 68: 9984-10007
China Pharmaceutical University
AI-Driven De Novo Design and Development of Nontoxic DYRK1A Inhibitors.
J Med Chem 68: 10346-10364
Instituto de Ciencias Matemeticas (ICMAT-CSIC)
PSMA-Guided PROTAC Degraders for Tumor-Specific Protein Degradation in Prostate Cancer.
J Med Chem 68: 10139-10155
Ocean University of China
Structural Optimization of Pyrazole Compounds as Hsp90 Regulators with Enhanced Antitumor Activity.
J Med Chem 68: 9886-9905
China Pharmaceutical University
Bardoxolone Derivatives as Novel Pseudo-Natural Necroptosis Inhibitors by Destabilizing HSP90 Client Proteins.
J Med Chem 68: 9906-9925
Second Military Medical University
Inverse Agonists of Peroxisome Proliferator-Activated Receptor Gamma: Advances and Prospects in Cancer Treatment.
J Med Chem 68: 9084-9100
Shenyang Pharmaceutical University
Discovery of ATX968: An Orally Available Allosteric Inhibitor of DHX9.
J Med Chem 68: 9537-9554
Accent Therapeutics, Inc.
Synthesis of 5,9- and 5,8-Diaminoalkoxy Substituted Benzophenanthridinone Analogues as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors and Their Radiosensitizing Activity.
J Med Chem 68: 9323-9340
Sun Yat-sen University
Design, Synthesis, and Biological Evaluation of Selective STING Synergists That Enhance cGAMP-STING Pathway Activation without Inherent Agonist Activity.
J Med Chem 68: 9407-9430
Beijing Institute of Pharmacology and Toxicology
Drug-like Antagonists of P2Y Receptor Subtypes: An Update.
J Med Chem 68: 9057-9083
University of Nottingham
Discovery of Potent PDEδ/NAMPT Dual Inhibitors: Preclinical Evaluation in KRAS Mutant Pancreatic Cancer Cells.
J Med Chem 68: 9241-9259
Shanghai University
Challenging triple negative breast cancer through HDAC6 selective inhibition: Novel cap-group identification, structure-activity relationships, computational and biological studies.
Eur J Med Chem 292:
University of Naples Federico II
Novel tacrine-based multi-target directed Ligands: Enhancing cholinesterase inhibition, NMDA receptor antagonism, and CNS bioavailability for Alzheimer's disease treatment.
Eur J Med Chem 292:
University Hospital Hradec Kralove
Toward Dual-Target Glycomimetics against Two Bacterial Lectins to Fight Pseudomonas aeruginosa-Burkholderia cenocepacia Infections: A Biophysical Study.
J Med Chem 68: 9681-9693
Universite degli Studi di Milano
Discovery and Optimization of a Covalent AKR1C3 Inhibitor.
J Med Chem 68: 9465-9478
University of Texas at Austin
Exploring Simple Drug Scaffolds from the Generated Database Chemical Space Reveals a Chiral Bicyclic Azepane with Potent Neuropharmacology.
J Med Chem 68: 9176-9201
University of Bern
Discovery of a Potent, Selective, and Brain-Penetrant Checkpoint Kinase 1 Inhibitor, BEN-28010, for the Treatment of Glioblastoma.
J Med Chem 68: 9101-9125
BenevolentAI
Redesigning oxazolidinones as carbonic anhydrase inhibitors against vancomycin-resistant enterococci.
Eur J Med Chem 291:
University of Florence
Derivatives of the Clinically Used HIF Prolyl Hydroxylase Inhibitor Desidustat Are Efficient Inhibitors of Human γ-Butyrobetaine Hydroxylase.
J Med Chem 68: 9777-9798
University of Oxford
On-Resin Assembly of Macrocyclic Inhibitors of Cryptococcus neoformans May1: A Pathway to Potent Antifungal Agents.
J Med Chem 68: 9623-9637
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
Synthesis and Pharmacological Characterization of Novel Peripheral Cannabinoid-1 Receptor Blockers Based on a Tricyclic Scaffold.
J Med Chem 68: 9431-9445
The Hebrew University of Jerusalem
Thienopyrimidinone Derivatives as a GluN2B/C/D Biased, Positive Allosteric Modulator of the N-Methyl-d-Aspartate Receptor.
J Med Chem 68: 9303-9322
Emory University
Synthetic approaches and clinical application of KRAS inhibitors for cancer therapy.
Eur J Med Chem 291:
Shengjing Hospital of China Medical University
Challenging the "Undruggable"─Targeting STAT3 but Identifying Potent TrkA-Targeted Inhibitors.
J Med Chem 68: 9501-9524
University of British Columbia
Structure-Guided Design of ISOX-DUAL-Based Degraders Targeting BRD4 and CBP/EP300: A Case of Degrader Collapse.
J Med Chem 68: 9638-9660
University of Sussex
1,5-Disubstituted 1,2,3-triazoles: Molecular scaffolds for medicinal chemistry and biomolecular mimetics.
Eur J Med Chem 291:
Indira Gandhi National Tribal University
Discovery of potent focal adhesion kinase (FAK) inhibitor A8 with enhanced antitumor activity.
Eur J Med Chem 291:
Beijing Normal University
Discovery and Optimization of Potent and Highly Selective PARP14 Inhibitors for the Treatment of Atopic Dermatitis.
J Med Chem 68: 9755-9776
China Pharmaceutical University
Discovery and Evaluation of Active Site-Directed, Potent, and Selective Sulfophenyl Acetic Amide-Based Inhibitors for the Laforin Phosphatase.
J Med Chem 68: 9220-9240
Purdue University
Ubiquitin-Specific Protease 7 (USP7) as a Promising Therapeutic Target for Drug Discovery: From Mechanisms to Therapies.
J Med Chem 68: 7914-7931
Zhengzhou University
Shooting an Arrow against Convulsion: Novel Triazole-Grafted Benzenesulfonamide Derivatives as Carbonic Anhydrase II and VII Inhibitors.
J Med Chem 68: 8873-8893
Horus University-Egypt
Identification of JNJ-61803534, a RORγt Inverse Agonist for the Treatment of Psoriasis.
J Med Chem 68: 8713-8728
Phenex Pharmaceuticals AG
Synthesis and Evaluation of Thiazolidinone-Isatin Hybrids for Selective Inhibition of Cancer-Related Carbonic Anhydrases.
ACS Med Chem Lett 16: 560-566
University of Cagliari
Novel Piperidinylpyridinylcarbonitrile Derivatives as QPCT and QPCTL Inhibitors for Treating Cancer.
ACS Med Chem Lett 16: 540-541
Smith, Gambrell & Russell
Design, Synthesis, and Evaluation of a New Fluorescent Ligand for the M2 Muscarinic Acetylcholine Receptor.
ACS Med Chem Lett 16: 552-559
HUN-REN Research Centre for Natural Sciences
Integrated Advancements in Neuroplasticity, Psychedelic Therapeutics, and AI-Driven Innovations for Precision Medicine.
ACS Med Chem Lett 16: 520-522
Usona Institute
1,6-Naphthridine Compounds as SMARCA2 Inhibitors for Treating Non-small Cell Lung Cancer.
ACS Med Chem Lett 16: 528-529
Smith, Gambrell & Russell
Targeting Oncogenic Pathways: Advances in KRAS, CDK, EGFR, and PROTAC-Based Therapies.
ACS Med Chem Lett 16: 523-525
Usona Institute
Novel PARP7 Inhibitors for Treating Cancer.
ACS Med Chem Lett 16: 526-527
Smith, Gambrell & Russell
Novel 6-Aryl isoindolin-1-one Derivatives as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 2.
ACS Med Chem Lett 16: 510-511
Emory University
Novel Compounds as NLRP3 Inhibitors for Treating Asthma or COPD.
ACS Med Chem Lett 16: 538-539
Smith, Gambrell & Russell
Discovery of Novel DDR1 Inhibitors through a Hybrid Virtual Screening Pipeline, Biological Evaluation and Molecular Dynamics Simulations.
ACS Med Chem Lett 16: 602-610
Tongde Hospital of Zhejiang Province
6-Aryl Isoindolin-1-ones: Novel mGluR2 Negative Allosteric Modulators.
ACS Med Chem Lett 16: 512-513
Emory University
Novel Cyclic Peptides as Interleukin-23 Inhibitor for Treating Inflammatory Disorders.
ACS Med Chem Lett 16: 532-533
Emory University
Design, synthesis and bioevaluation of novel hydrazide derivatives as enhancers of immunotherapy and DNA-damage response in antitumor therapy.
Eur J Med Chem 291:
Gannan Medical University
Discovery of a Potent and Selective Protein Arginine Methyltransferase 5 (PRMT5) PROTAC Degrader.
J Med Chem 68: 8543-8563
Icahn School of Medicine at Mount Sinai
Discovery of Novel Bifunctional Agents as Potent Androgen Receptor Antagonists and Degraders for the Treatment of Enzalutamide-Resistant Prostate Cancer.
J Med Chem 68: 8330-8345
China Pharmaceutical University
Tertiary Alcohol: Reaping the Benefits but Minimizing the Drawbacks of Hydroxy Groups in Drug Discovery.
J Med Chem 68: 7889-7913
Takeda Pharmaceuticals
Discovery of Dual PD-L1/HDAC3 Inhibitors for Tumor Immunotherapy.
J Med Chem 68: 8046-8064
Southern Medical University
Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4.
J Med Chem 68: 8933-8966
The University of Melbourne
Discovery of Phenylacylpiperidine as Novel sEH Inhibitors through Scaffold Hopping of Natural Stilbene.
J Med Chem 68: 8980-9013
Beijing Institute of Technology
Identification of Novel Cyclobutane-Based Derivatives as Potent Acetyl-CoA Carboxylase Allosteric Inhibitors for Nonalcoholic Steatohepatitis Drug Discovery.
J Med Chem 68: 8578-8599
Nanjing Sanhome Pharmaceutical Co. Ltd.
Efficacy and Toxicity Analysis of Selective BET Bromodomain Inhibitors in Models of Inflammatory Liver Disease.
J Med Chem 68: 8091-8105
University of Minnesota
PCSK9 Targeted Autophagosome-Tethering Compounds: Design, Synthesis, and Antiatherosclerosis Evaluation.
J Med Chem 68: 8190-8207
Fudan University
Development of Novel PRMT7 Inhibitors for the Treatment of Prostate Cancer.
J Med Chem 68: 8244-8268
China Pharmaceutical University
Bifunctional Inhibition of Botulinum Neurotoxin A Protease: Unexpected Active Site Inhibition Enhances Covalent Targeting of an Allosteric Site.
J Med Chem 68: 8796-8816
The Scripps Research Institute
Discovery and exploration of disubstituted [1,2,5]oxadiazolo-[3,4-b]pyrazines as novel C-C chemokine receptor type 5 signaling inhibitors targeting the intracellular allosteric binding pocket.
Eur J Med Chem 291:
KU Leuven
Design, synthesis, and biological evaluation of quinolinyl-ureido-phenyl-hydrazide derivatives and quinolinyl-hydrazide derivatives as anticancer agents targeting Nur77-mediated ferroptosis.
Eur J Med Chem 291:
Xiamen University
Discovery of Novel TYRO3/MERTK Dual Inhibitors.
J Med Chem 68: 8455-8470
University of North Carolina at Chapel Hill
Rational Design of Methylene Blue-Raloxifene Conjugates for Efficient Breast Tumor Elimination Triggered by ERα Degradation.
J Med Chem 68: 8861-8872
Guizhou University
Discovery of FLT3-ITD Inhibitor Clifutinib: A Novel Biphenylacetylene Urea Derivative in Clinical Trials for the Treatment of Relapsed/Refractory FLT3-ITD+ Acute Myeloid Leukemia.
J Med Chem 68: 7955-7972
Sunshine Lake Pharma Company, Ltd.
Discovery of non-electrophilic TRPA1 channel agonists with anti-nociceptive effects via rapid current desensitization.
Eur J Med Chem 291:
Qingdao University Medical College
Discovery of WEE1 Kinase Inhibitors with Potent Activity against Patient-Derived, Metastatic Colorectal Cancer Organoids.
J Med Chem 68: 8065-8090
Monash University (Parkville Campus)
Selective Inhibition of Rat α7 Nicotinic Acetylcholine Receptors by LvID, a Newly Characterized α4/7-Conotoxin from Conus lividus.
J Med Chem 68: 8163-8173
Zhejiang University
Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation.
J Med Chem 68: 8634-8647
Icahn School Of Medicine At Mount Sinai
Discovery of 2,4-dianilinopyrimidine derivatives as novel p90 ribosomal S6 protein kinase (RSK) inhibitors.
Eur J Med Chem 291:
Changzhi University
Discovery of a Novel Dihydroisoquinolinone Derivative as a Potent CDK9 Inhibitor Capable of Overcoming L156F Mutant for the Treatment of Hematologic Malignancies.
J Med Chem 68: 8106-8123
Hefei Institutes of Physical Science
Discovery of Naphthyridinone Derivatives as Selective and Potent PKMYT1 Inhibitors with Antitumor Efficacy.
J Med Chem 68: 8497-8515
China Innovation Center of Roche
Structure-Based Discovery Targeting GSK-3α Reveals Potent Nanomolar Selective 4-Phenyl-1H-benzofuro[3,2-b]pyrazolo[4,3-e]pyridine Inhibitor with Promising Glioblastoma and CNS-Active Potential in Cellular Models.
J Med Chem 68: 8679-8693
University of Central Lancashire
Lead Optimization of Positive Allosteric KV7.2/3 Channel Modulators toward Improved Balance of Lipophilicity and Aqueous Solubility.
J Med Chem 68: 8377-8399
University of Greifswald
Development of Squaramides as Allosteric Modulators of the CB1 Receptor: Synthesis, Computational Studies, Biological Characterization, and Effects against Cocaine-Induced Behavioral Sensitization and Reinstatement in Rats.
J Med Chem 68: 8694-8712
Research Triangle Institute
Novel Spiro-Barbiturates Can Reverse the Action of General Anesthetics on the GABAAR.
J Med Chem 68: 8025-8045
University of Illinois Chicago
Development of Hydrazide-Based HDAC6 Selective Inhibitors for Treating NLRP3 Inflammasome-Related Diseases.
J Med Chem 68: 9279-9302
Ocean University of China
Design, Synthesis, and Biological Evaluation of Pyrrolo[1,2-a]quinoxalin-4(5H)-one Derivatives as Potent and Orally Available Noncovalent Bruton's Tyrosine Kinase (BTK) Inhibitors.
J Med Chem 68: 8841-8860
East China University of Science and Technology
Discovery of Potent STING Inhibitors Bearing a Difluorobenzodioxol Structural Motif as Potent Anti-Inflammatory Agents.
J Med Chem 68: 8907-8932
Shanghai Jiao Tong University
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting.
Eur J Med Chem 291:
University of Padova
Accelerating the Hit-To-Lead Optimization of a SARS-CoV-2 Mpro Inhibitor Series by Combining High-Throughput Medicinal Chemistry and Computational Simulations.
J Med Chem 68: 8269-8294
Idorsia Pharmaceuticals Limited
Deuteration Strategy-Inspired Design of Novel Diarylpyrimidine Derivatives as Potent Non-Nucleoside Reverse Transcriptase Inhibitors Featuring Improved Efficacy, Selectivity, and Druggability.
J Med Chem 68: 8564-8577
Fudan University
Structure-Based Design and Optimization Lead to the Identification of a Novel Potent sEH Inhibitor with PPARγ Partial Agonist Activity against Inflammatory and Metabolic-Related Diseases.
J Med Chem 68: 8729-8767
Shenyang Pharmaceutical University
The Liebeskind-Srogl cross-coupling reaction towards the synthesis of biologically active compounds.
Eur J Med Chem 290:
Palacky University
Exploiting structural variability in the kinase back-pocket to modulate polypharmacology of TAM inhibitors.
Eur J Med Chem 290:
University of North Carolina at Chapel Hill
Synthesis and structure-activity evaluation of a series of novel tricyclic STING activators.
Eur J Med Chem 290:
Curadev Pharma Pvt. Ltd.
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII.
Eur J Med Chem 290:
"G. d'Annunzio" University of Chieti-Pescara
Discovery of a series of novel 3-sulfonamido benzoic acid derivatives as promising P2Y14R antagonists for acute lung injury.
Eur J Med Chem 290:
Zhengzhou University
HDAC11 Inhibition as a Potential Therapeutic Strategy for AML: Target Identification, Lead Discovery, Antitumor Potency, and Mechanism Investigation.
J Med Chem 68: 8124-8142
Shandong University
Acetal functionalized iminosugars for targeting β-glucocerebrosidase modulation.
Eur J Med Chem 290:
"Ugo Schiff" (DICUS)
TCM theory-inspired discovery of DNJ-flavonoid conjugates as broad-spectrum anti-SARS-CoV-2 agents by primarily targeting ER-associated glycoprotein folding process.
Eur J Med Chem 290:
Central South University
Design of Novel Mercapto-3-phenylpropanoyl Dipeptides as Dual Angiotensin-Converting Enzyme C-Domain-Selective/Neprilysin Inhibitors.
J Med Chem 68: 7720-7736
University of Bath
Indolizine Derivatives Inhibit TRPM2 and Protect against Ischemic Brain Injury with an Extended Treatment Window.
J Med Chem 68: 7642-7661
Zhejiang University
Synthesis and biological evaluation of novel 4-Arylaminoquinolines derivatives as EGFR/HDAC inhibitors.
Bioorg Med Chem Lett 122:
Beijing University of Technology
Discovery of novel transforming growth factor β type 1 receptor inhibitors through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation in hepatocellular carcinoma.
Bioorg Med Chem 123:
Tianjin Medical University
From N-0385 to N-0920: Unveiling a Host-Directed Protease Inhibitor with Picomolar Antiviral Efficacy against Prevalent SARS-CoV-2 Variants.
J Med Chem 68: 7119-7136
University of Sherbrooke
Real Way to Target Gram-Negative Pathogens: Discovery of a Novel Helicobacter pylori Antibiotic Class.
J Med Chem 68: 10128-10138
The University of Iowa College of Pharmacy
Reversible Small Molecule Multivariant Ras Inhibitors Display Tunable Affinity for the Active and Inactive Forms of Ras.
J Med Chem 68: 9129-9161
CRUK Scotland Institute
Rational Design of the First Dual Agonist at Trace Amine-Associated Receptor 1 and 5-HT2C Receptors Based on Binding Pocket Similarity for the Treatment of Schizophrenia and Alzheimer's Disease-Related Psychosis.
J Med Chem 68: 7082-7105
Yantai University
Design, synthesis, and activity evaluation of novel STING inhibitors based on C170 and H151.
Eur J Med Chem 290:
Ocean University of China
From Bones to Bugs: Structure-Based Development of Raloxifene-Derived Pathoblockers That Inhibit Pyocyanin Production in Pseudomonas aeruginosa.
J Med Chem 68: 7390-7420
Technische Universitat Braunschweig
Discovery of phenylisoxazolidine analogs targeting receptor interacting protein kinase 1 with anti-inflammatory activity.
Eur J Med Chem 290:
China Pharmaceutical University
A highly active angiotensin I-converting enzyme inhibitory peptide KAKW designed based on the role of C-terminal residue, and its antihypertensive effects on spontaneously hypertensive rats.
Eur J Med Chem 290:
East China University of Science and Technology
Design, Synthesis, Evaluation, and SAR of 5-Phenylisoindoline Derivatives, a Potent Class of Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 (PD-1/PD-L1) Interaction.
J Med Chem 68: 7291-7312
Capital Medical University
Discovery of the 2,3-Dihydrobenzopyrane-4-one as a Potent FTO Inhibitor against Obesity-Related Metabolic Diseases.
J Med Chem 68: 7421-7440
Anhui Medical University
Discovery of 4-((quinolin-8-ylthio)methyl)benzamide derivatives as a new class of SARS-CoV-2 nsp13 inhibitors.
Bioorg Med Chem Lett 122:
Sichuan University
Synthesis and biological activity of 1H-pyrrolo[3,2-g]isoquinolines as Haspin kinase inhibitors.
Bioorg Med Chem 123:
Universite Clermont Auvergne
Discovery of AMG 193, an MTA-Cooperative PRMT5 Inhibitor for the Treatment of MTAP-Deleted Cancers.
J Med Chem 68: 6932-6954
Amgen Inc.
Towards P2X4 Positron Emission Tomography Tracing.
J Med Chem 68: 6961-6964
University of Trieste
Potent and Selective Human Constitutive Androstane Receptor Activator DL5055 Facilitates Cyclophosphamide-Based Chemotherapies.
J Med Chem 68: 7044-7061
University of Maryland
Discovery of Highly Potent AKR1C3 Inhibitors Treating Sorafenib-Resistant Hepatocellular Carcinoma.
J Med Chem 68: 7367-7389
China Pharmaceutical University
Design, synthesis, molecular docking and ADME of novel phenylalanine derivatives as mushroom tyrosinase inhibitors.
Bioorg Med Chem Lett 122:
Sun Yat-sen University
Design, synthesis and biological evaluation of 3-amino-6-(2-hydroxyphenyl)pyridazin-4-aryl derivatives as SMARCA2/4 degraders.
Eur J Med Chem 290:
Sichuan University
Discovery of novel azetidine-based imidazopyridines as selective and orally bioavailable inhibitors of phosphodiesterase 10A for the treatment of pulmonary arterial hypertension.
Eur J Med Chem 290:
Sun Yat-sen University
PaAP-Activatable NIR Probe for Diagnosing, Imaging, and Discovering Small-Molecule Therapeutics against Implant-Associated Biofilm Infections.
J Med Chem 68: 7827-7838
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of Conformationally Constrained Dihydro Benzo-Indole Derivatives as Metallo-β-Lactamase Inhibitors to Tackle Multidrug-Resistant Bacterial Infections.
J Med Chem 68: 7062-7081
CSIR-Institute of Microbial Technology
Deconstruction of Dual-Site Tankyrase Inhibitors Provides Insights into Binding Energetics and Suggests Critical Hotspots for Ligand Optimization.
J Med Chem 68: 7263-7279
University of Oulu
Development of acylhydrazone linked thiazoles as non-covalent dual inhibitors of SARS-CoV-2 proteases.
Eur J Med Chem 290:
CSIR-Indian Institute of Chemical Technology
Novel 15-lipoxygenase-1 inhibitor protects cells from RSL3-induced cell death.
Eur J Med Chem 290:
University of Groningen
Discovery and rational optimization of 2, 2'-((1H-indole-2,3-diyl) bis (thio))diacetamide as novel SARS-CoV-2 RdRp inhibitors.
Bioorg Med Chem 123:
Chinese Academy of Medical Science and Peking Union Medical College
Discovery of Potent and Balanced Dual RIPK2 and 3 Inhibitors as a New Strategy for the Treatment of Inflammatory Bowel Diseases.
J Med Chem 68: 7539-7559
Anhui Medical University
Uncovering α-Selectivity for Liver X Receptor Agonists for Lipotoxic Cancer Therapies.
J Med Chem 68: 7180-7196
University of Tuebingen
Discovery of c-Kit as a New Therapeutic Target in LPS-Induced Acute Lung Injury through Novel Phenylamide Derivative D9.
J Med Chem 68: 7499-7517
Wenzhou Medical University
Development of Tricyclic 4,5-Dihydro-3H-pyrrolo[2,3-c]quinolin-4-ones as Potent Autotaxin Inhibitors for Pulmonary Fibrosis Treatment In Vivo.
J Med Chem 68: 7476-7498
Shenyang Pharmaceutical University
Rational design, optimization, and biological evaluation of novel pyrrolo-pyridone derivatives as potent and orally active Cbl-b inhibitors.
Eur J Med Chem 290:
Tsinghua University
6,7-Dimethoxy-2-methyl-4-substituted quinazolines: Design, synthesis, EGFR inhibitory activity, in vitro cytotoxicity, and in silico studies.
Eur J Med Chem 290:
Egyptian Drug Authority (EDA)
Macrocyclic dihydropyridine analogs as pan-BET BD2-preferred inhibitors.
Eur J Med Chem 290:
University of Minnesota
Discovery of first-in-class human glycolate oxidase near infrared molecular rotor inhibitors (NIRGOi).
Eur J Med Chem 290:
Newcastle University
Discovery of a Highly Potent and Selective Tyrosine Kinase 2 (TYK2) Degrader with In Vivo Therapeutic Efficacy in a Murine Psoriasis Model.
J Med Chem 68: 7560-7578
China Pharmaceutical University
Discovery of a novel quinoxaline derivative modulator via a dual P53/TLR2 targeting strategy for the alleviation of radiation damage.
Eur J Med Chem 290:
Beijing Institute of Radiation Medicine
Design, synthesis and biological evaluation of WEE1 degraders via HSP90-mediated targeting chimeras for target therapy of acute myeloid leukemia.
Eur J Med Chem 290:
East China Normal University
Discovery of Novel SIK2/3 Inhibitors for the Potential Treatment of MEF2C+ Acute Myeloid Leukemia (AML).
J Med Chem 68: 7518-7538
Insilico Medicine Shanghai Ltd.
Chemoproteomic Profiling of C. albicans for Characterization of Antifungal Kinase Inhibitors.
J Med Chem 68: 7615-7629
University of North Carolina at Chapel Hill
A Hybrid Energy-Based and AI-Based Screening Approach for the Discovery of Novel Inhibitors of AXL.
ACS Med Chem Lett 16: 410-419
Hangzhou Medical College
Discovery of HM-279, a Potent Inhibitor of ALK5 for Improving Therapeutic Efficacy of Cancer Immunotherapy.
J Med Chem 68: 7106-7118
Carna Biosciences, Inc.
Discovery of ATP competitive PDHK1/2 dual inhibitors.
Bioorg Med Chem Lett 122:
China Innovation Center of Roche
Discovery of potent and selective CDK2 inhibitors with high safety and favorable bioavailability for the treatment of cancer.
Eur J Med Chem 290:
China Pharmaceutical University
Discovery of HMPL-306 (Ranosidenib), a New Potent and Selective Dual Inhibitor of Mutant IDH1 and 2 in Clinical Development for Cancer Treatment.
ACS Med Chem Lett 16: 454-463
HUTCHMED Limited
Development of Ethyl-Hydrazide-Based Selective Histone Deacetylase 6 (HDAC6) PROTACs.
ACS Med Chem Lett 16: 487-495
University of Bonn
Is a Fungal Apocalypse Inevitable or Just a Hallucination? An Overview of the Antifungal Armamentarium Used in the Fight against Pathogenic Fungi.
ACS Med Chem Lett 16: 379-387
Charles Sturt University
In-Silico Screening-Based Discovery of New Natural eEF2K Inhibitors with Neuritogenic Activity.
ACS Med Chem Lett 16: 475-482
Jinan University
Novel Cyclic Peptides Inhibiting Tumor Necrosis Factor Receptor 1 Activity.
ACS Med Chem Lett 16: 363-365
Emory University
Derivatives of Aristoquinoline Accessed through a Ritter-like Reaction.
ACS Med Chem Lett 16: 406-409
University of Illinois Chicago
Identification of Indazole- and Azaindazole-Substituted Cyclopentapyrroles as G2019S Leucine-Rich Repeat Kinase 2 Inhibitors for the Treatment of CNS Disorders.
ACS Med Chem Lett 16: 368-370
Emory University
Novel Pyrimidinyl Sulfonamide Derivatives as GPR17 Modulators.
ACS Med Chem Lett 16: 361-362
Emory University
Novel 5,6-Fused and 6,6-Fused Bicyclic Compounds as 15-Prostaglandin Dehydrogenase Modulators.
ACS Med Chem Lett 16: 366-367
Emory University
Peripherally Restricted Fused Heterocyclic Peptidomimetic Multifunctional Opioid Agonists as Novel, Potent Analgesics.
ACS Med Chem Lett 16: 388-396
University of Florida
Thiosulfonate-Based Targeted Covalent Cruzipain Inhibitors with Enhanced Bioactivity Translation for Antichagasic Therapy.
ACS Med Chem Lett 16: 464-474
Universidad Nacional de Cordoba (FCQ-UNC)
Identification of Phosphodiesterase-7 Inhibitors with Spiro[[1,3]oxazolo[5,4-f]quinazoline-9,1'-cyclohexan]-7-one Scaffold for the Treatment of Chronic Fatigue.
ACS Med Chem Lett 16: 356-357
Emory University
Structural Studies of the Dopamine D4 Receptor Antagonist Sonepiprazole as an Inhibitor of Human Carbonic Anhydrases.
ACS Med Chem Lett 16: 483-486
University of Florence
Exploiting Solvent Exposed Salt-Bridge Interactions for the Discovery of Potent Inhibitors of SOS1 Using Free-Energy Perturbation Simulations.
ACS Med Chem Lett 16: 444-453
Schrodinger, Inc.
From DNA-Encoded Library Screening to AM-9747: An MTA-Cooperative PRMT5 Inhibitor with Potent Oral In Vivo Efficacy.
J Med Chem 68: 6534-6557
Amgen Inc
Discovery of dual CDK4/6 and BRD4 inhibitor as apoptosis and autophagy inducers against NSCLC in vitro and in vivo.
Eur J Med Chem 290:
China Pharmaceutical University
Design, synthesis and biological evaluation of 2-[1-(pyridin-2-ylmethyl)-1H-pyrazole-3-carboxamido]benzoic acids as promising urate transporter 1 inhibitors with potential nephroprotective efficacy for the treatment of hyperuricemic nephropathy.
Eur J Med Chem 290:
Shenyang Pharmaceutical University
Unveiling a novel pyrazolopyrimidine scaffold as a dual COX-2/5-LOX inhibitor with immunomodulatory potential: Design, synthesis, target prediction, anti-inflammatory activity, and ADME-T with docking simulation.
Eur J Med Chem 290:
Al-Azhar University
Phenyl-benzyl-ureas with pyridazinone motif: Potent soluble epoxide hydrolase inhibitors with enhanced pharmacokinetics and efficacy in a paclitaxel-induced neuropathic pain model.
Eur J Med Chem 290:
Gazi University
Designing Macrocyclic Kinase Inhibitors Using Macrocycle Scaffold Hopping with Reinforced Learning (Macro-Hop).
J Med Chem 68: 6698-6717
Jinan University
Discovery of a Potent SARM1 Base-Exchange Inhibitor with In Vivo Efficacy.
J Med Chem 68: 6558-6575
Roche Pharma Research and Early Development
Discovery of BT-114143, a Novel and Potent Phosphoric Acid-Containing Small-Molecule Plasminogen Activation Inhibitor for Hyperfibrinolysis.
J Med Chem 68: 6084-6099
ScinnoHub Pharmaceutical Co., Ltd.
Size-Dependent Target Engagement of Covalent Probes.
J Med Chem 68: 6616-6632
HUN-REN Research Centre for Natural Sciences
Design, Biological Characterization, and Discovery of Capromorelin Derivatives as Oral Growth Hormone Secretagogue Receptor Type 1a Agonist for the Treatment of Growth Hormone Deficiency.
J Med Chem 68: 6766-6788
Changchun Genescience Pharma
Aromatic nitroolefin with inhibition efficacy in triple-negative breast cancer cells by dual targeting RXRα and tubulins.
Eur J Med Chem 289:
Xiamen University
Recent advances in CDC7 kinase inhibitors: Novel strategies for the treatment of cancers and neurodegenerative diseases.
Eur J Med Chem 289:
Sichuan University
Design, synthesis, and biological evaluation of novel aminopyrimidine derivatives as EGFR inhibitors.
Bioorg Med Chem Lett 122:
Jiangnan University
A new potent and selective peroxisome proliferator-activated receptor alpha partial agonist displays anti-steatotic effects In vitro and behaves as a safe hypolipidemic and hypoglycemic agent in a diabetic mouse model.
Eur J Med Chem 289:
University of Bari
Synthesis, screening and validation of cysteine-reactive fragments as chikungunya virus protease inhibitors.
Bioorg Med Chem Lett 122:
Australian National University
Design, synthesis, and biological evaluation of 4-(2-fluorophenoxy)pyridine derivatives as novel FLT3-ITD inhibitors.
Eur J Med Chem 289:
Guizhou Provinc
Discovery of YJZ5118: A Potent and Highly Selective Irreversible CDK12/13 Inhibitor with Synergistic Effects in Combination with Akt Inhibition.
J Med Chem 68: 6718-6734
Shanghai Institute of Organic Chemistry
Optimization of Cyclophilin B-Targeted Tri-vector Inhibitors for Novel MASH Treatments.
J Med Chem 68: 6815-6831
University of Edinburgh
Discovery, synthesis, and biological mechanism evaluation of novel quinoline derivatives as potent NLRP3 inhibitors.
Eur J Med Chem 289:
Guangzhou Medical University
AI-Driven Discovery of Highly Specific and Efficacious hCES2A Inhibitors for Ameliorating Irinotecan-Triggered Gut Toxicity.
J Med Chem 68: 6252-6269
Hainan University
UNC9426, a Potent and Orally Bioavailable TYRO3-Specific Inhibitor.
J Med Chem 68: 6665-6682
University of North Carolina at Chapel Hill
Discovery of novel dihydropteridone derivatives as orally bioavailable PLK1 inhibitors with reduced hERG inhibitory activity for acute myeloid leukemia treatment.
Eur J Med Chem 289:
Shenyang Pharmaceutical University
Structure-activity relationship analysis of meta-substituted N-cyclopropylmethyl-nornepenthones with mixed KOR/MOR activities.
Eur J Med Chem 289:
Fudan University
Structure-Based Optimization of Moracin M as Potent and Selective PDE4 Inhibitors with Antipsoriasis Effects.
J Med Chem 68: 6789-6803
Hainan University
Monoselective Histone Deacetylase 6 PROTAC Degrader Shows In Vivo Tractability.
J Med Chem 68: 6165-6177
University of Toronto Mississauga
Total Synthesis of (-)- and (+)-Talaroenamine B and Diphenylene Derivatives.
J Nat Prod 88: 842-849
Henan Polytechnic University
A comprehensive review of fused imidazonaphthyridine derivatives: Synthetic approaches and biological applications.
Bioorg Med Chem 122:
Monash University Malaysia
Cross-subclass metallo-β-lactamase inhibitors: From structural and catalytic commonalities guiding design.
Eur J Med Chem 289:
Beijing University of Chemical Technology
Discovery of Daraxonrasib (RMC-6236), a Potent and Orally Bioavailable RAS(ON) Multi-selective, Noncovalent Tri-complex Inhibitor for the Treatment of Patients with Multiple RAS-Addicted Cancers.
J Med Chem 68: 6064-6083
Revolution Medicines, Inc.
Discovery of novel benzoxazole analogues as potential anticancer agent selectively targeting aromatase.
Bioorg Med Chem 122:
Commerce and Science College
Design, synthesis and biological evaluation of novel hydroxamic acid-derived histone deacetylase inhibitors bearing a 2-oxoindoline scaffold as potential antitumor agents.
Bioorg Med Chem 122:
Hanoi University of Pharmacy
Discovery of New Azaindole Metallo-Deubiquitinase CSN5 Inhibitors.
J Med Chem 68: 6748-6765
Xihua University
An Amazing 30-Year Journey around the DABO Family: A Medicinal Chemistry Lesson on a Versatile Class of Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors.
J Med Chem 68: 5993-6026
Sapienza University of Rome
Structure-based design of novel 2,4,5-trisubstituted pyrimidine derivatives as potent HIV-1 NNRTIs by exploiting the tolerant regions in NNTRIs binding pocket.
Eur J Med Chem 289:
Shandong University
Synthesis and Biological Evaluation of Peripheral 5HT2B Antagonists for Liver Fibrosis.
J Med Chem 68: 6493-6506
Jeonbuk National University Medical School
Discovery of Novel, Potent, Orally Bioavailable and Efficacious, Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors for Hematopoietic Stem Cell Mobilization.
J Med Chem 68: 6386-6406
FibroGen Inc.
Discovery of 5-Phenylthiazol-2-amine Derivatives as Novel PI4KIIIβ Inhibitors with Efficacious Antitumor Activity by Inhibiting the PI3K/AKT Axis.
J Med Chem 68: 6270-6291
China Pharmaceutical University
Structure-Based Development of 3,4-Fused Tricyclic Benzofuran Derivatives as Polyketide Synthase 13 Inhibitors with Negligible hERG Inhibition.
J Med Chem 68: 6312-6327
East China Normal University
Dual Modulator of FXR and HSD17B13: Revitalizing FXR Therapies in MASH.
J Med Chem 68: 6104-6107
The Fifth Affiliated Hospital of Guangxi Medical University & The First People's Hospital of Nanning
Impact of fixed phosphorus position on activity of triazole bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Bioorg Med Chem 122:
University of Iowa
The Heterogeneous Kinetic Origins of the Binding Properties of Orthosteric Ligands at Heteromeric Nicotinic Acetylcholine Receptors.
J Med Chem 68: 6683-6697
University of Copenhagen
Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor.
J Med Chem 68: 6292-6311
Sapienza University of Rome
DNA-Encoded Library Screen Identifies Novel Series of Respiratory Syncytial Virus Polymerase Inhibitors.
J Med Chem 68: 6407-6430
Johnson & Johnson Company
Discovery and Optimization of Novel Apo-IDO1 Inhibitors by a Pharmacophore-Based Structural Simplification Strategy.
J Med Chem 68: 6633-6655
China Pharmaceutical University
Discovery of Isobenzofuran-1(3H)-one Derivatives as Selective TREK-1 Inhibitors with In Vitro and In Vivo Neuroprotective Effects.
J Med Chem 68: 5804-5823
Chinese Academy of Medical Sciences and Peking Union Medical College
Combination therapy and dual-target inhibitors based on cyclin-dependent kinases (CDKs): Emerging strategies for cancer therapy.
Eur J Med Chem 289:
Southwest Jiaotong University
Discovery of a potent and in vivo anti-inflammatory Efficacious, P2Y14R antagonist with a novel benzisoxazoles scaffold by DNA-encoded chemical library technology.
Eur J Med Chem 289:
Zhengzhou University
Anti-inflammatory agents design via the fragment hybrid strategy in the discovery of compound c1 for treating ALI and UC.
Eur J Med Chem 289:
Wenzhou Medical University
MrgX2-Targeting Ligand Screen for Antipseudoallergic Agents by Immobilized His-Tag-Fused Protein Technology.
J Med Chem 68: 5942-5953
Xi'an Jiaotong University
Discovery of DFV890, a Potent Sulfonimidamide-Containing NLRP3 Inflammasome Inhibitor.
J Med Chem 68: 5529-5550
IFM Therapeutics GmbH
Development of Potent SHP2 Allosteric Inhibitors: Design, Synthesis, and Evaluation with Antitumor Effects.
J Med Chem 68: 5238-5256
Peking University
Discovery of TNG462: A Highly Potent and Selective MTA-Cooperative PRMT5 Inhibitor to Target Cancers with MTAP Deletion.
J Med Chem 68: 5097-5119
Tango Therapeutics
Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors.
J Med Chem 68: 5760-5773
Michigan State University
Discovery of Potent and Selective MNK Kinase Inhibitors for the Treatment of Leukemia.
J Med Chem 68: 5824-5844
Northwestern University
Discovery of Novel 2,4,5-Trisubstituted Pyrimidine Derivatives as Potent and Selective FGFR Inhibitors against Gatekeeper Mutants for the Treatment of NSCLC.
J Med Chem 68: 5907-5925
Wenzhou Medical University
Discovery of the Clinical Candidate YY2201 as a Highly Potent and Selective ATR Inhibitor.
J Med Chem 68: 5292-5311
Chinese Academy of Medical Sciences & Peking Union Medical College
Design, synthesis and biological evaluation of pyrrolopyrimidine urea derivatives as novel KRASG12C inhibitors for the treatment of cancer.
Eur J Med Chem 289:
Nanjing Tech University
Design, synthesis and activity evaluation of 4-(quinoline-2-yl)aniline derivatives as SARS-CoV‑2 main protease inhibitors.
Bioorg Med Chem 121:
Macau University of Science and Technology
Integrated computational and biosensor-based strategies for the discovery of allosteric SMYD3 ligands using diperodon as a starting point.
Bioorg Med Chem 121:
Uppsala University
Discovery of novel tranylcypromine-indazole-based derivatives as LSD1 inhibitors for acute myeloid leukemia treatment.
Eur J Med Chem 289:
Zhengzhou University
Development of 3-arylaminothiophenic-2-carboxylic acid derivatives as new FTO inhibitors showing potent antileukemia activities.
Eur J Med Chem 289:
University of Chinese Academy of Sciences
Novel gut-restricted bivalent agonists targeting mucosal 5-HT4R: Design, synthesis, and biological evaluation.
Eur J Med Chem 289:
Shanghai Institute of Pharmaceutical Industry Co., Ltd.
Design and Synthesis of Novel Deazapurine DNMT 1 Inhibitors with In Vivo Efficacy in DLBCL.
J Med Chem 68: 5333-5357
Sichuan University
The discovery of novel N-heterocyclic-based AKT inhibitors with potential efficacy against prostate cancer.
Eur J Med Chem 289:
Shandong University
Research progress of LpxC inhibitor on Gram-negative bacteria.
Eur J Med Chem 289:
Minzu University of China
Design, synthesis and optimization of Apcin analogues as Cdc20 inhibitors for triple-negative breast cancer therapy.
Eur J Med Chem 289:
Central South University
Structural Optimization of Covalent Inhibitors for Deubiquitinase ChlaDUB1 of Chlamydia trachomatis as Antibiotic Agents.
J Med Chem 68: 5400-5425
Julius-Maximilians-Universitat Wurzburg (JMU)
Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease.
J Med Chem 68: 7003-7030
Pfizer Inc.
Structure-Based Design of New LSD1/EGFRL858R/T790M Dual Inhibitors for Treating EGFR Mutant NSCLC Cancers.
J Med Chem 68: 5954-5972
Zhengzhou University
Asiatic acid and its derivatives: Pharmacological insights and applications.
Eur J Med Chem 289:
Shenyang Pharmaceutical University
Design and synthesis of azole derivatives of echinocystic acid as α-glucosidase inhibitors with hypoglycemic activity.
Eur J Med Chem 289:
Yanbian University
Discovery of highly potent AKR1Cs pan-inhibitors as chemotherapeutic potentiators to restore breast cancer drug resistance.
Eur J Med Chem 289:
China Pharmaceutical University
Design, synthesis and biological activity of 8-hydroxy modified urolithin A derivatives as phosphodiesterase type II (PDE2) inhibitors.
Bioorg Med Chem 121:
Changzhou University
Design, synthesis, and biological evaluation of novel azaspirooxindolinone derivatives as potent inhibitors of ITK and BTK-dependent cancers.
Bioorg Med Chem 121:
GITAM University
Orally Bioavailable and Site-Selective Covalent STING Inhibitor Derived from a Macrocyclic Marine Diterpenoid.
J Med Chem 68: 5471-5487
National Health Research Institutes
Novel Hypochlorous Acid-Activated Near-Infrared Probe Monitors the Dynamic Changes of Myeloperoxidase Activity in Ischemic Brain.
J Med Chem 68: 5382-5399
Nanjing Medical University
Discovery, Synthesis, and Activity Evaluation of Novel Small-Molecule Inhibitors Targeting VISTA for Cancer Immunotherapy.
J Med Chem 68: 5222-5237
China Pharmaceutical University
Discovery of Novel Pyrrolo[2,3-b]pyridine-Based CSF-1R Inhibitors with Demonstrated Efficacy against Patient-Derived Colorectal Cancer Organoids.
J Med Chem 68: 5655-5674
Nanjing University of Chinese Medicine
Discovery of a Novel 1,4-Benzodiazepine Derivative as a Highly Selective ANXA3 Degrader for the Treatment of Triple-Negative Breast Cancer.
J Med Chem 68: 5358-5381
Fudan University
Discovery of Novel Oxazolo[4,3-f]purine Derivatives as Antitumor Agents through PPIA Interaction.
J Med Chem 68: 5573-5596
Henan Normal University
Multi-Water Bridges Enable Design of BET BD1-Selective Inhibitors for Pancreatic Cancer Therapy.
J Med Chem 68: 5719-5735
China Pharmaceutical University
Furazanopyrazine-based novel promising anticancer agents interfering with the eicosanoid biosynthesis pathways by dual mPGES-1 and sEH inhibition.
Eur J Med Chem 289:
University of Salerno
Discovery of potent, highly selective, and orally bioavailable factor XIa inhibitors for anticoagulant therapy.
Eur J Med Chem 289:
Hefei University of Technology
Design, synthesis, and antitumor activity of NSDs inhibitors targeting lung squamous cell carcinoma.
Eur J Med Chem 289:
Peking University
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