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Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors.
J Med Chem 67: 2-16 (0)
The State University of New York
Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.
J Med Chem 67: 17-37 (2024)
National Research Council of Italy
Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles.
J Med Chem 67: 38-64 (0)
Joint Research Institution of Altitude Health and Institute of Respiratory Health and National Clinical Research Center for Geriatrics
Discovery of Novel Inhibitors of BRD4 for Treating Prostate Cancer: A Comprehensive Case Study for Considering Water Networks in Virtual Screening and Drug Design.
J Med Chem 67: 138-151 (0)
Zhejiang University
Discovery of Potent and Selective Phosphatidylinositol 3-Phosphate 5-Kinase (PIKfyve) Inhibitors as Methuosis Inducers.
J Med Chem 67: 165-179 (0)
Sichuan University/West China School of Nursing
Discovery of 2-Ethoxy-5-isobutyramido-N-1-substituted Benzamide Derivatives as Selective Kv2.1 Inhibitors with In Vivo Neuroprotective Effects.
J Med Chem 67: 213-233 (0)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery, Optimization, and Evaluation of Potent and Selective DNA-PK Inhibitors in Combination with Chemotherapy or Radiotherapy for the Treatment of Malignancies.
J Med Chem 67: 245-271 (0)
West China Hospital
Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.
J Med Chem 67: 322-348 (0)
China Pharmaceutical University
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
J Med Chem 67: 380-401 (2024)
Galapagos
Fragment Merging, Growing, and Linking Identify New Trypanothione Reductase Inhibitors for Leishmaniasis.
J Med Chem 67: 402-419 (2024)
Sapienza University of Rome
Discovery of Tetrahydropyrazolopyrazine Derivatives as Potent and Selective MYT1 Inhibitors for the Treatment of Cancer.
J Med Chem 67: 420-432 (0)
Insilico Medicine Shanghai Ltd
Targeted Degradation of PCSK9 In Vivo by Autophagy-Tethering Compounds.
J Med Chem 67: 433-449 (0)
Fudan University
Lead Optimization of BIBR1591 To Improve Its Telomerase Inhibitory Activity: Design and Synthesis of Novel Four Chemical Series with In Silico, In Vitro, and In Vivo Preclinical Assessments.
J Med Chem 67: 492-512 (0)
Horus University-Egypt
Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior.
J Med Chem 67: 529-542 (0)
University of Illinois Chicago
Identification of a Sonically Activated Degrader of Methionine Adenosyltransferase 2A by an in Silico Approach Assisted with the Hole-Electron Analysis.
J Med Chem 67: 543-554 (0)
Guizhou University
Design and Discovery of Novel NLRP3 Inhibitors and PET Imaging Radiotracers Based on a 1,2,3-Triazole-Bearing Scaffold.
J Med Chem 67: 555-571 (0)
Virginia Commonwealth University
Electrophilic MiniFrags Revealed Unprecedented Binding Sites for Covalent HDAC8 Inhibitors.
J Med Chem 67: 572-585 (2024)
Hun-Ren Research Centre for Natural Sciences
Molecular Pharmacology Profiling of Phenylfentanil and Its Analogues to Understand the Putative Involvement of an Adrenergic Mechanism in Fentanyl-Induced Respiratory Depression.
J Med Chem 67: 603-619 (0)
Virginia Commonwealth University
Exploiting the Carboxylate-Binding Pocket of β-Lactamase Enzymes Using a Focused DNA-Encoded Chemical Library.
J Med Chem 67: 620-642 (0)
Baylor College of Medicine
Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist.
J Med Chem 67: 643-673 (0)
Gedeon Richter Plc
Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3.
J Med Chem 67: 674-690 (0)
Goethe University Frankfurt
Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile.
J Med Chem 67: 709-727 (0)
National Institute on Drug Abuse - Intramural Research Program
Discovery of 4-Ethoxy-6-chloro-5-azaindazoles as Novel PDE4 Inhibitors for the Treatment of Alcohol Use Disorder and Alcoholic Liver Diseases.
J Med Chem 67: 728-753 (0)
Southern Medical University
From Hit to Lead: Structure-Based Optimization of Novel Selective Inhibitors of Receptor-Interacting Protein Kinase 1 (RIPK1) for the Treatment of Inflammatory Diseases.
J Med Chem 67: 754-773 (0)
Sichuan University
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
J Med Chem 67: 774-781 (2024)
Mirati Therapeutics
Unraveling the Puzzle of Therapeutic Peptides: A Promising Frontier in Huntington's Disease Treatment.
J Med Chem 67: 783-815 (0)
Aligarh Muslim University
Rising Star in Immunotherapy: Development and Therapeutic Potential of Small-Molecule Inhibitors Targeting Casitas B Cell Lymphoma-b (Cbl-b).
J Med Chem 67: 816-837 (0)
China Pharmaceutical University
Emerging Drug Targets for Antimalarial Drug Discovery: Validation and Insights into Molecular Mechanisms of Function.
J Med Chem 67: 838-863 (0)
University of Zambia
Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.
J Med Chem 67: 864-884 (2024)
Astrazeneca
Hepatitis C: The Story of a Long Journey through First, Second, and Third Generation NS3/4A Peptidomimetic Inhibitors. What Did We Learn?
J Med Chem 67: 885-921 (0)
Ri.MED Foundation
Combination Therapy and Dual-Target Inhibitors Based on LSD1: New Emerging Tools in Cancer Therapy.
J Med Chem 67: 922-951 (0)
Zhengzhou University
Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development.
J Med Chem 67: 952-970 (0)
Japan Tobacco
Dual Antagonism of α9α10 nAChR and GABAB Receptor-Coupled CaV2.2 Channels by an Analgesic αO-Conotoxin Analogue.
J Med Chem 67: 971-987 (0)
Ocean University of China
Discovery of Novel Aminobutanoic Acid-Based ASCT2 Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.
J Med Chem 67: 988-1007 (0)
China Pharmaceutical University
Development of Antibacterial Peptides with Membrane Disruption and Folate Pathway Inhibitory Activities against Methicillin-Resistant Staphylococcus aureus.
J Med Chem 67: 1044-1060 (0)
Qilu University of Technology (Shandong Academy of Sciences)
Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase.
J Med Chem 67: 1061-1078 (2024)
Imperial College London
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.
J Med Chem 67: 1079-1092 (0)
Nanjing University of Chinese Medicine
Ligand-Based Competition Binding by Real-Time
J Med Chem 67: 1115-1126 (2024)
University of Bologna
Structure-Guided Design, Synthesis, and Antivirulence Assessment of Covalent Staphylococcus aureus Sortase A Inhibitors.
J Med Chem 67: 1127-1146 (0)
Nanjing University of Chinese Medicine
Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRASG12D.
J Med Chem 67: 1147-1167 (0)
Shanghai Institute of Materia Medica
Discovery, Optimization, and Evaluation of Novel Pyridin-2(1H)-one Analogues as Potent TRK Inhibitors for Cancer Treatment.
J Med Chem 67: 1168-1183 (0)
Shanghai Tech University
Discovery of Natural Ah Receptor Antagonists from Salvia miltiorrhiza Bunge and Synthesis of Analogs for Tumor Immunotherapy.
J Med Chem 67: 1243-1261 (0)
Chinese Academy of Medical Sciences and Peking Union Medical College
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
J Med Chem 67: 1262-1313 (0)
Arvinas LLC
Discovery of Novel and Potent Prolyl Hydroxylase Domain-Containing Protein (PHD) Inhibitors for The Treatment of Anemia.
J Med Chem 67: 1393-1405 (0)
Insilico Medicine Shanghai Ltd
Discovery of TP0628103: A Highly Potent and Selective MMP-7 Inhibitor with Reduced OATP-Mediated Clearance Designed by Shifting Isoelectric Points.
J Med Chem 67: 1406-1420 (0)
Taisho Pharmaceutical Co., Ltd.
Structure-Activity Relationships and Discovery of (S)-6-Isopropyl-2-methoxy-3-(3-methoxypropoxy)-10-oxo-5,10-dihydro-6H-pyrido[1,2-h][1,7]naphthyridine-9-carboxylic Acid (AB-452), a Novel Orally Available HBV RNA Destabilizer.
J Med Chem 67: 1421-1446 (0)
Arbutus Biopharma
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
J Med Chem 67: 1447-1459 (0)
Novartis Institutes for Biomedical Research
Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.
J Med Chem 67: 1460-1480 (0)
Stanford University
Discovery of the First-in-Class RORγ Covalent Inhibitors for Treatment of Castration-Resistant Prostate Cancer.
J Med Chem 67: 1481-1499 (0)
Sun Yat-Sen University
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
J Med Chem 67: 1500-1512 (0)
AstraZeneca
Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.
J Med Chem 67: 1513-1532 (0)
China Pharmaceutical University
Discovery of Potent, Orally Bioavailable, Tricyclic NLRP3 Inhibitors.
J Med Chem 67: 1544-1562 (0)
Novartis Biomedical Research
Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo.
J Med Chem 67: 1563-1579 (0)
East China University of Science and Technology
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
J Med Chem 67: 1580-1610 (2024)
Jagiellonian University Medical College
Discovery of Novel Pyridazine-Tethered Sulfonamides as Carbonic Anhydrase II Inhibitors for the Management of Glaucoma.
J Med Chem 67: 1611-1623 (0)
Tanta University
Peptide-Drug Conjugates: An Emerging Direction for the Next Generation of Peptide Therapeutics.
J Med Chem 67: 1641-1661 (0)
University of Illinois Chicago
SIRT3 Activation a Promise in Drug Development? New Insights into SIRT3 Biology and Its Implications on the Drug Discovery Process.
J Med Chem 67: 1662-1689 (0)
Sapienza University of Rome
Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research.
J Med Chem 67: 1701-1733 (0)
Bristol-Myers Squibb Company
Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
J Med Chem 67: 1734-1746 (0)
Kinnate Biopharma
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
J Med Chem 67: 1747-1757 (0)
Kinnate Biopharma
Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization.
J Med Chem 67: 1758-1782 (0)
University of Siena
Specific Inhibitors of Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity.
J Med Chem 67: 1843-1860 (0)
University of Bayreuth
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis.
J Med Chem 67: 1914-1931 (0)
Zhejiang University
Discovery of Highly Selective PARP7 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
J Med Chem 67: 1932-1948 (0)
China Pharmaceutical University
Rebamipide and Derivatives are Potent, Selective Inhibitors of Histidine Phosphatase Activity of the Suppressor of T Cell Receptor Signaling Proteins.
J Med Chem 67: 1949-1960 (0)
University of Minnesota
Tight-Binding Small-Molecule Carboxylesterase 2 Inhibitors Reduce Intracellular Irinotecan Activation.
J Med Chem 67: 2019-2030 (0)
University of Toronto Mississauga
Multitargeting HDAC Inhibitors Containing a RAS/RAF Protein Interfering Unit.
J Med Chem 67: 2066-2082 (0)
Southeast University
Discovery of Artemisinins as Microsomal Prostaglandins Synthase-2 Inhibitors for the Treatment of Colorectal Cancer via Chemoproteomics.
J Med Chem 67: 2083-2094 (0)
Changshu Institute of Technology
Design and Synthesis of Dual-Targeting Inhibitors of sEH and HDAC6 for the Treatment of Neuropathic Pain and Lipopolysaccharide-Induced Mortality.
J Med Chem 67: 2095-2117 (0)
Shenyang Pharmaceutical University
Structure-Guided Design of a Highly Potent Partial RXR Agonist with Superior Physicochemical Properties.
J Med Chem 67: 2152-2164 (0)
Ludwig-Maximilians-Universitat (LMU) Munchen
Discovery and Characterization of a Bicyclic Peptide (Bicycle) Binder to Thymic Stromal Lymphopoietin.
J Med Chem 67: 2220-2235 (0)
BicycleTx Limited
Fragment-to-Lead Medicinal Chemistry Publications in 2022.
J Med Chem 67: 2287-2304 (0)
Astex Pharmaceuticals
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
J Med Chem 67: 2321-2336 (2024)
Nurix Therapeutics
Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500).
J Med Chem 67: 2349-2368 (0)
Repare Therapeutics, Inc.
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
J Med Chem 67: 2369-2378 (2024)
Calibr At Scripps Research Institute
Discovery of the Novel, Orally Active, and Selective LPA1 Receptor Antagonist ACT-1016-0707 as a Preclinical Candidate for the Treatment of Fibrotic Diseases.
J Med Chem 67: 2397-2424 (0)
Idorsia Pharmaceuticals, Ltd
Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases.
J Med Chem 67: 2438-2465 (0)
The People's Hospital of Guangxi Zhuang Autonomous Region & Guangxi Academy of Medical Sciences
Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma.
J Med Chem 67: 2466-2486 (0)
Fudan University
A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRASG12C Inhibitor.
J Med Chem 67: 2487-2511 (0)
Ocean University of China
Identifying Marine-Derived Tanzawaic Acid Derivatives as Novel Inhibitors against Osteoclastogenesis and Osteoporosis via Downregulation of NF-κB and NFATc1 Activation.
J Med Chem 67: 2602-2618 (0)
Chinese Academy of Sciences
PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
J Med Chem 67: 2619-2630 (2024)
Unidad Bics
Discovery and Characterization of Selective, First-in-Class Inhibitors of Citron Kinase.
J Med Chem 67: 2631-2666 (0)
Lerner Research Institute
Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J Med Chem 67: 2667-2689 (0)
Jinan University
Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.
J Med Chem 67: 2712-2731 (0)
University of Illinois at Chicago
Design, Synthesis, and Biological Evaluation for First GPX4 and CDK Dual Inhibitors.
J Med Chem 67: 2758-2776 (0)
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Dual Inhibitors of EGFRL858R/T790M/ACK1 to Overcome Osimertinib Resistance in Nonsmall Cell Lung Cancers.
J Med Chem 67: 2777-2801 (0)
Sichuan University
Discovery of a Novel Series of Homo sapiens Caseinolytic Protease P Agonists for Colorectal Adenocarcinoma Treatment via ATF3-Dependent Integrated Stress Response.
J Med Chem 67: 2812-2836 (0)
Sichuan University
ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases.
J Med Chem 67: 2837-2848 (0)
Stanford University
Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma.
J Med Chem 67: 2884-2906 (0)
Shanghai Institute of Materia Medica
BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor.
J Med Chem 67: 2907-2940 (0)
Bayer AG
Identification of Piperazinyl-Difluoro-indene Derivatives Containing Pyridyl Groups as Potent FGFR Inhibitors against FGFR Mutant Tumor: Design, Synthesis, and Biological Evaluation.
J Med Chem 67: 2941-2962 (0)
Peking Union Medical College and Chinese Academy of Medical Sciences
First-in-Class Dual EZH2-HSP90 Inhibitor Eliciting Striking Antiglioblastoma Activity
J Med Chem 67: 2963-2985 (2024)
Taipei Medical University
Discovery of 2,3-Diaminoindole Derivatives as a Novel Class of NOD Antagonists.
J Med Chem 67: 3004-3017 (0)
University of Naples "Federico II"
Synthetic Approaches to Novel Human Carbonic Anhydrase Isoform Inhibitors Based on Pyrrol-2-one Moiety.
J Med Chem 67: 3018-3038 (2024)
Romanian Academy
Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.
J Med Chem 67: 3039-3065 (0)
Symeres
Novel Carbonic Anhydrase Inhibitors with Dual-Tail Core Sulfonamide Show Potent and Lasting Effects for Glaucoma Therapy.
J Med Chem 67: 3066-3089 (0)
University of Florence
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
J Med Chem 67: 3090-3111 (0)
AstraZeneca
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.
J Med Chem 67: 3112-3126 (0)
Incyte
Exploring the Function of (+)-Naltrexone Precursors: Their Activity as TLR4 Antagonists and Potential in Treating Morphine Addiction.
J Med Chem 67: 3127-3143 (0)
Chinese Academy of Sciences
Discovery of D25, a Potent and Selective MNK Inhibitor for Sepsis-Associated Acute Spleen Injury.
J Med Chem 67: 3167-3189 (0)
Shandong First Medical University
Antiviral Protein-Protein Interaction Inhibitors.
J Med Chem 67: 3205-3231 (2024)
Wroclaw University
Unleashing the Potential of Camptothecin: Exploring Innovative Strategies for Structural Modification and Therapeutic Advancements.
J Med Chem 67: 3244-3273 (0)
Southwest Jiaotong University
Structural Basis for Molecular Recognition of Cannabinoids by Inhibitory Cys-Loop Channels.
J Med Chem 67: 3274-3286 (0)
Universidad de Buenos Aires
Degradation of Polo-like Kinase 1 by the Novel Poly-Arginine N-Degron Pathway PROTAC Regulates Tumor Growth in Nonsmall Cell Lung Cancer.
J Med Chem 67: 3307-3320 (0)
Korea Basic Science Institute (KBSI)
Heterocyclic-Modified Imidazoquinoline Derivatives: Selective TLR7 Agonist Regulates Tumor Microenvironment against Melanoma.
J Med Chem 67: 3321-3338 (0)
Southern Medical University
Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer.
J Med Chem 67: 3339-3357 (0)
National Institute of Pharmaceutical Education and Research-Ahmedabad (NIPER-A)
Design, Synthesis, and Biological Evaluation of Pierardine Derivatives as Novel Brain-Penetrant and In Vivo Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
J Med Chem 67: 3358-3384 (0)
Anhui University of Chinese Medicine
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
J Med Chem 67: 3400-3418 (0)
Merck & Co.
Design and Synthesis of Dual-Target Inhibitors Targeting Androgen Receptors and Glucocorticoid Receptors to Overcome Antiandrogen Resistance in Castration-Resistant Prostate Cancer.
J Med Chem 67: 3419-3436 (0)
Zhejiang Normal University
Discovery of Effective Dual PROTAC Degraders for Neurodegenerative Disease-Associated Aggregates.
J Med Chem 67: 3448-3466 (0)
Sun Yat-sen University
Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment.
J Med Chem 67: 3504-3519 (0)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis.
J Med Chem 67: 3571-3589 (0)
Bristol Myers Squibb
Design, Synthesis, and Antitumor Activity Evaluation of Novel VISTA Small Molecule Inhibitors.
J Med Chem 67: 3590-3605 (0)
China Pharmaceutical University
Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors.
J Med Chem 67: 3606-3625 (0)
China Pharmaceutical University
Discovery of 5-Hydroxy-1,4-naphthoquinone (Juglone) Derivatives as Dual Effective Agents Targeting Platelet-Cancer Interplay through Protein Disulfide Isomerase Inhibition.
J Med Chem 67: 3626-3642 (2024)
National Taiwan University
Discovery of Novel Steroid-Based Histamine H3 Receptor Antagonists/Inverse Agonists.
J Med Chem 67: 3643-3667 (0)
Gedeon Richter Plc.
Hit-to-Lead Identification and Validation of a Triaromatic Pleuromutilin Antibiotic Candidate.
J Med Chem 67: 3692-3710 (0)
University of Southern Denmark
Optimization Efforts for Identification of Novel Highly Potent Keap1-Nrf2 Protein-Protein Interaction Inhibitors.
J Med Chem 67: 3741-3763 (0)
Japan Tobacco
Rational Design of Benzobisheterocycle Metallo-β-Lactamase Inhibitors: A Tricyclic Scaffold Enhances Potency against Target Enzymes.
J Med Chem 67: 3795-3812 (0)
University of the Republic (UdelaR)
Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors.
J Med Chem 67: 3813-3842 (0)
Goethe University Frankfurt
Discovery of Novel N-(Anthracen-9-ylmethyl) Benzamide Derivatives as ZNF207 Inhibitors Promising in Treating Glioma.
J Med Chem 67: 3909-3934 (0)
China Pharmaceutical University
Structure-Based Discovery of High-Affinity Small Molecule Ligands and Development of Tool Probes to Study the Role of Chitinase-3-Like Protein 1.
J Med Chem 67: 3959-3985 (0)
Molecure
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
J Med Chem 67: 3986-4006 (0)
Shanghai Institute of Materia Medica
Discovery of Highly Potent Small-Molecule PD-1/PD-L1 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
J Med Chem 67: 4083-4099 (0)
China Pharmaceutical University
Discovery and Characterization of a New Class of C5aR1 Antagonists Showing In Vivo Activity.
J Med Chem 67: 4100-4119 (0)
Idorsia Pharmaceuticals
Discovery of a Potent Nicotinamide Phosphoribosyltransferase Activator for Improving Aging-associated Dysfunctions.
J Med Chem 67: 4120-4130 (0)
Second Military Medical University (Naval Medical University)
Discovery and Structure-Activity Relationships of Novel ssDAF-12 Receptor Modulators.
J Med Chem 67: 4150-4169 (0)
University of Perugia
Dual Inhibitors of Brain Carbonic Anhydrases and Monoamine Oxidase-B Efficiently Protect against Amyloid-β-Induced Neuronal Toxicity, Oxidative Stress, and Mitochondrial Dysfunction.
J Med Chem 67: 4170-4193 (0)
University of Florence
Discovery of RORγ Allosteric Fluorescent Probes and Their Application: Fluorescence Polarization, Screening, and Bioimaging.
J Med Chem 67: 4194-4224 (0)
Nanjing University of Chinese Medicine
Glycan-Modified Peptides for Dual Inhibition of Human Immunodeficiency Virus Entry into Dendritic Cells and T Cells.
J Med Chem 67: 4225-4233 (0)
Chinese Academy of Sciences
RNA-Small-Molecule Interaction: Challenging the "Undruggable" Tag.
J Med Chem 67: 4259-4297 (0)
Panjab University
Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations.
J Med Chem 67: 4346-4375 (0)
Nanjing University of Chinese Medicine
Identification of Novel Series of Potent and Selective Relaxin Family Peptide Receptor 1 (RXFP1) Agonists.
J Med Chem 67: 4442-4462 (0)
AstraZeneca
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate.
J Med Chem 67: 4525-4540 (2024)
University of Oxford
Development of a Series of Pyrrolopyridone MAT2A Inhibitors.
J Med Chem 67: 4541-4559 (0)
AstraZeneca
Design and Synthesis of 3-(2H-Chromen-3-yl)-5-aryl-1,2,4-oxadiazole Derivatives as Novel Toll-like Receptor 2/1 Agonists That Inhibit Lung Cancer In Vitro and In Vivo.
J Med Chem 67: 4583-4602 (0)
Beijing Institute of Radiation Medicine
Structure-Guided Discovery of Potent and Selective CLK2 Inhibitors for the Treatment of Knee Osteoarthritis.
J Med Chem 67: 4603-4623 (0)
China Pharmaceutical University
Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs.
J Med Chem 67: 4641-4654 (0)
Imperial College London
Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2).
J Med Chem 67: 4655-4675 (0)
Astex Pharmaceuticals
The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
J Med Chem 67: 4676-4690 (0)
Biogen
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
J Med Chem 67: 4691-4706 (2024)
Max Planck Institute of Molecular Physiology
Discovery of Conformationally Constrained ALK2 Inhibitors.
J Med Chem 67: 4707-4725 (0)
Ontario Institute for Cancer Research
Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation.
J Med Chem 67: 4739-4756 (0)
Shenyang Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus.
J Med Chem 67: 4757-4781 (0)
Sichuan University
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation.
J Med Chem 67: 4819-4832 (0)
Genentech
Mechanism-Based Macrocyclic Inhibitors of Serine Proteases.
J Med Chem 67: 4833-4854 (0)
Washington University School of Medicine
Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model.
J Med Chem 67: 4855-4869 (0)
Shanghai University of Traditional Chinese Medicine
Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury.
J Med Chem 67: 4889-4903 (0)
Fujian University of Traditional Chinese Medicine
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
J Med Chem 67: 4916-4935 (0)
China Pharmaceutical University
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
J Med Chem 67: 4936-4949 (2024)
Mirati Therapeutics
Design, Synthesis, and Structure-Activity Relationship of Novel Pyridazinone-Based PARP7/HDACs Dual Inhibitors for Elucidating the Relationship between Antitumor Immunity and HDACs Inhibition.
J Med Chem 67: 4950-4976 (0)
Hangzhou Normal University
Discovery of Novel PD-L1 Small-Molecular Inhibitors with Potent In Vivo Anti-tumor Immune Activity.
J Med Chem 67: 4977-4997 (0)
China Pharmaceutical University
Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability.
J Med Chem 67: 5032-5052 (0)
Shandong University
Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor.
J Med Chem 67: 5093-5108 (0)
Novartis Pharma AG
Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins.
J Med Chem 67: 5144-5167 (0)
Sichuan University
Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications.
J Med Chem 67: 5185-5215 (0)
Sichuan University
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
J Med Chem 67: 5216-5232 (2024)
Galapagos
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
J Med Chem 67: 5233-5258 (2024)
Galapagos
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
J Med Chem 67: 5259-5271 (0)
Pharmaron UK Ltd.
Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression.
J Med Chem 67: 5275-5304 (0)
University of Michigan
Discovery of Novel 11-Membered Templates as Squalene Synthase Inhibitors.
J Med Chem 67: 5305-5314 (0)
Daiichi Sankyo RD Novare Co., Ltd.
Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer.
J Med Chem 67: 5351-5372 (0)
University of Michigan
Design, Synthesis, and Activity Evaluation of Fluorine-Containing Scopolamine Analogues as Potential Antidepressants.
J Med Chem 67: 5391-5420 (0)
Henan Normal University
5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein-Protein Interaction-Derived Functions.
J Med Chem 67: 5421-5436 (0)
University of Helsinki
Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma.
J Med Chem 67: 5437-5457 (0)
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of a Novel NIK Inhibitor with Anti-Inflammatory and Hepatoprotective Effects for Sepsis Treatment.
J Med Chem 67: 5617-5641 (0)
China Pharmaceutical University
Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease.
J Med Chem 67: 5642-5661 (0)
Nanjing University of Chinese Medicine
Discovery of Novel 5,6-Dihydro-4H-pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases.
J Med Chem 67: 5662-5682 (0)
Beijing University of Technology
Discovery of DNL343: A Potent, Selective, and Brain-Penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases.
J Med Chem 67: 5758-5782 (0)
Denali Therapeutics Inc.
Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy.
J Med Chem 67: 5783-5799 (0)
Tongji University
Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.
J Med Chem 67: 5837-5853 (0)
Icahn School of Medicine At Mount Sinai
Model of P-Glycoprotein Ligand Binding and Validation with Efflux Substrate Matched Pairs.
J Med Chem 67: 5854-5865 (2024)
University of California
Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors.
J Med Chem 67: 5866-5882 (0)
University of North Carolina
Long-Residence Time Peptide Antagonist for the Vasopressin V2 Receptor to Treat Autosomal Dominant Polycystic Kidney Disease.
J Med Chem 67: 5935-5944 (0)
Xuzhou Medical University
Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.
J Med Chem 67: 5963-5998 (0)
Shenyang Pharmaceutical University
Channeling Nicotinamide Phosphoribosyltransferase (NAMPT) to Address Life and Death.
J Med Chem 67: 5999-6026 (0)
University of Arizona
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises.
J Med Chem 67: 6052-6063 (0)
TU Dortmund University and Drug Discovery Hub Dortmund (DDHD)
Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers.
J Med Chem 67: 6064-6080 (0)
Tango Therapeutics
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.
J Med Chem 67: 6099-6118 (0)
Tianjin University
Synthesis and Structure-Activity Relationships for Glutamate Transporter Allosteric Modulators.
J Med Chem 67: 6119-6143 (0)
Drexel University College of Medicine
Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist.
J Med Chem 67: 6144-6188 (0)
Cybin IRL Limited
Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy.
J Med Chem 67: 6253-6267 (0)
The Sixth Affiliated Hospital of Wenzhou Medical University
Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3'-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury.
J Med Chem 67: 6268-6291 (0)
Shanghai Jiao Tong University
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.
J Med Chem 67: 6313-6326 (0)
Zhejiang Sci-Tech University
Allosteric Activation of α7 Nicotinic Acetylcholine Receptors by Novel 2-Arylamino-thiazole-5-carboxylic Acid Amide Derivatives for the Improvement of Cognitive Deficits in Mice.
J Med Chem 67: 6344-6364 (0)
Qingdao University Medical College
Structure-Guided Discovery and Preclinical Assessment of Novel (Thiophen-3-yl)aminopyrimidine Derivatives as Potent ERK1/2 Inhibitors.
J Med Chem 67: 6425-6455 (0)
Sichuan University
Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.
J Med Chem 67: 6495-6507 (0)
Texas A&M University
Discovery of 2-Amide-3-methylester Thiophenes that Target SARS-CoV-2 Mac1 and Repress Coronavirus Replication, Validating Mac1 as an Antiviral Target.
J Med Chem 67: 6519-6536 (0)
University of Oulu
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles.
J Med Chem 67: 6549-6569 (0)
Eberhard Karls University Tubingen
Discovery of Novel Aryl Triazolone Dihydropyridines (ATDPs) Targeting Highly Conserved Residue W229 as Promising HIV-1 NNRTIs.
J Med Chem 67: 6570-6584 (0)
Shandong University
Potentiating Activity of GmhA Inhibitors on Gram-Negative Bacteria.
J Med Chem 67: 6610-6623 (0)
Mutabilis
Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia.
J Med Chem 67: 6638-6657 (0)
Zhejiang University
Peptide Inhibitor Targeting the Extraterminal Domain in BRD4 Potently Suppresses Breast Cancer Both In Vitro and In Vivo.
J Med Chem 67: 6658-6672 (0)
Xiamen University
Discovery of Highly Potent Solute Carrier 13 Member 5 (SLC13A5) Inhibitors for the Treatment of Hyperlipidemia.
J Med Chem 67: 6687-6704 (0)
China Pharmaceutical University
Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity.
J Med Chem 67: 6769-6792 (0)
Sichuan University
Butyrylcholinesterase-Activated Near-Infrared Fluorogenic Probe for In Vivo Theranostics of Alzheimer's Disease.
J Med Chem 67: 6793-6809 (0)
China Pharmaceutical University
Discovery of a Novel CSF-1R Inhibitor with Highly Improved Pharmacokinetic Profiles and Superior Efficacy in Colorectal Cancer Immunotherapy.
J Med Chem 67: 6854-6879 (0)
Nanjing University of Chinese Medicine
Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader.
J Med Chem 67: 6880-6892 (0)
Icahn School of Medicine At Mount Sinai
Psychoplastogenic DYRK1A Inhibitors with Therapeutic Effects Relevant to Alzheimer's Disease.
J Med Chem 67: 6922-6937 (0)
University of California
Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader.
J Med Chem 67: 6938-6951 (0)
Shanghai Institute of Organic Chemistry
Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity.
J Med Chem 67: 6952-6986 (0)
Guangzhou Institutes of Biomedicine and Health
Development of Benziodarone Analogues with Enhanced Potency for Selective Binding to Transthyretin in Human Plasma.
J Med Chem 67: 6987-7005 (0)
University of Toyama
Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors.
J Med Chem 67: 7048-7067 (0)
Center for Free-Electron Laser Science CFEL
Druglike, 18F-labeled PET Tracers Targeting Fibroblast Activation Protein.
J Med Chem 67: 7068-7087 (0)
University of Antwerp
Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect.
J Med Chem 67: 7112-7129 (0)
Fudan University
Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer.
J Med Chem 67: 7130-7145 (0)
China Pharmaceutical University
Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease.
J Med Chem 67: 7146-7157 (0)
Florida International University
Development of Prolinol Containing Inhibitors of Hypoxanthine-Guanine-Xanthine Phosphoribosyltransferase: Rational Structure-Based Drug Design.
J Med Chem 67: 7158-7175 (0)
The University of Queensland
Discovery of Urea Derivatives of Celastrol as Selective Peroxiredoxin 1 Inhibitors against Colorectal Cancer Cells.
J Med Chem 67: 7176-7196 (0)
Shanghai Jiao Tong University
Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists.
J Med Chem 67: 7224-7244 (0)
University of Copenhagen
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
J Med Chem 67: 7245-7259 (0)
University of Oxford
Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound.
J Med Chem 67: 7260-7275 (0)
Hangzhou Normal University
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation.
J Med Chem 67: 7283-7300 (0)
China Pharmaceutical University
Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer.
J Med Chem 67: 7330-7358 (0)
Guizhou Medical University
Discovery of a New Anti-Inflammatory Agent from Anemoside B4 Derivatives and Its Therapeutic Effect on Colitis by Targeting Pyruvate Carboxylase.
J Med Chem 67: 7385-7405 (0)
Soochow University
Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles.
J Med Chem 67: 7406-7430 (0)
Tanta University
Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.
J Med Chem 67: 7516-7538 (0)
Sichuan University
Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents.
J Med Chem 67: 7585-7602 (0)
Wenzhou Medical University
Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects.
J Med Chem 67: 7603-7619 (0)
Vrije Universiteit Brussel
Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors.
J Med Chem 67: 7620-7634 (0)
Central South University
Concurrent Optimizations of Efficacy and Blood-Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson's Disease Therapeutics.
J Med Chem 67: 7647-7662 (0)
Korea Advanced Institute of Science and Technology (KAIST)
Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update.
J Med Chem 67: 7668-7758 (0)
Eberhard Karls University Tubingen
Selenization of Small Molecule Drugs: A New Player on the Board.
J Med Chem 67: 7759-7787 (0)
University of Navarra
Triazoles in Medicinal Chemistry: Physicochemical Properties, Bioisosterism, and Application.
J Med Chem 67: 7788-7824 (0)
China Pharmaceutical University
Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility.
J Med Chem 67: 7825-7835 (0)
Cytokinetics, Inc.
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.
J Med Chem 67: 7836-7858 (0)
BeiGene(Beiing) Co., Ltd.
Cardiac Troponin Activator CK-963 Increases Cardiac Contractility in Rats.
J Med Chem 67: 7859-7869 (0)
Cytokinetics, Inc.
Discovery of Oral AMP-Activated Protein Kinase Activators for Treating Hyperlipidemia.
J Med Chem 67: 7870-7890 (0)
Chinese Academy of Medical Sciences and Peking Union Medical College
A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo.
J Med Chem 67: 7921-7934 (0)
Xiamen University
Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell.
J Med Chem 67: 7935-7953 (0)
Leiden University
A β-Carboline Derivate PAD4 Inhibitor Reshapes Neutrophil Phenotype and Improves the Tumor Immune Microenvironment against Triple-Negative Breast Cancer.
J Med Chem 67: 7973-7994 (0)
Capital Medical University
Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy.
J Med Chem 67: 7995-8019 (0)
Southern Medical University
Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases.
J Med Chem 67: 8060-8076 (0)
Hangzhou Medical College
Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases.
J Med Chem 67: 8077-8098 (0)
Idorsia Pharmaceuticals Ltd.
Design of FK866-Based Degraders for Blocking the Nonenzymatic Functions of Nicotinamide Phosphoribosyltransferase.
J Med Chem 67: 8099-8121 (0)
Beijing University of Chinese Medicine
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
J Med Chem 67: 8122-8140 (0)
Biogen Research and Development
Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches.
J Med Chem 67: 8141-8160 (0)
Novartis
Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer.
J Med Chem 67: 8161-8171 (0)
Insilico Medicine Shanghai Ltd
Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1.
J Med Chem 67: 8172-8185 (0)
University of California Riverside
Impact of Combinatorial Histone Modifications on Acetyllysine Recognition by the ATAD2 and ATAD2B Bromodomains.
J Med Chem 67: 8186-8200 (0)
University of Vermont
Exploring the Structural Attributes of Yoda1 for the Development of New-Generation Piezo1 Agonist Yaddle1 as a Vaccine Adjuvant Targeting Optimal T Cell Activation.
J Med Chem 67: 8225-8246 (0)
CSIR-Indian Institute of Chemical Biology
Discovery of Glutamate Carboxypeptidase III Ligands to Compete the Uptake of [177Lu]Lu-PSMA-617 in Healthy Organs.
J Med Chem 67: 8247-8260 (0)
Philochem
Design, Synthesis, and Evaluation of Dihydropyrimidine Derivatives as Selective PDE1 Inhibitors for the Treatment of Liver Fibrosis.
J Med Chem 67: 8309-8322 (0)
Hainan University
Structure-Activity Relationships toward the Identification of a High-Potency Selective Human Toll-like Receptor-7 Agonist.
J Med Chem 67: 8346-8360 (0)
Panjab University
Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation.
J Med Chem 67: 8383-8395 (0)
Biogen Inc.
Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity.
J Med Chem 67: 8406-8419 (0)
Wuyi University
Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma.
J Med Chem 67: 8445-8459 (0)
Sungkyunkwan University
Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.
J Med Chem 67: 8545-8568 (0)
Galapagos NV
An Improved PDE6D Inhibitor Combines with Sildenafil To Inhibit KRAS Mutant Cancer Cell Growth.
J Med Chem 67: 8569-8584 (0)
University of Luxembourg
Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.
J Med Chem 67: 8585-8608 (0)
Genentech
Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
J Med Chem 67: 8609-8629 (0)
Universidade Estadual de Campinas
Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation.
J Med Chem 67: 8642-8666 (0)
University of Florida
Discovery of Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation.
J Med Chem 67: 8667-8692 (0)
China Pharmaceutical University
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
J Med Chem 67: 8708-8729 (0)
Genentech
X-ray Structure-Guided Discovery of a Potent Benzimidazole Glutaminyl Cyclase Inhibitor That Shows Activity in a Parkinson's Disease Mouse Model.
J Med Chem 67: 8730-8756 (0)
Sichuan University
Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs.
J Med Chem 67: 8757-8790 (0)
University of Bonn
Development of Novel Phosphonodifluoromethyl-Containing Phosphotyrosine Mimetics and a First-In-Class, Potent, Selective, and Bioavailable Inhibitor of Human CDC14 Phosphatases.
J Med Chem 67: 8817-8835 (0)
Purdue University
Discovery and Optimization of Tetrahydroisoquinoline Derivatives To Enhance Lysosome Biogenesis as Preclinical Candidates for the Treatment of Alzheimer's Disease.
J Med Chem 67: 8836-8861 (0)
Nanjing University of Chinese Medicine
Illuminating Dark Chemical Matter Using the Cell Painting Assay.
J Med Chem 67: 8862-8876 (0)
Max-Planck Institute Institute of Molecular Physiology
Design of Selective PARP-1 Inhibitors and Antitumor Studies.
J Med Chem 67: 8877-8901 (0)
Shandong University
Discovery of Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer.
J Med Chem 67: 8913-8931 (0)
Zhongnan Hospital of Wuhan University
Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches.
J Med Chem 67: 8962-8987 (0)
AstraZeneca
Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
J Med Chem 67: 8988-9027 (0)
AstraZeneca
In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel.
J Med Chem 67: 9124-9149 (0)
University of Messina
WLB-87848, a Selective σ1 Receptor Agonist, with an Unusually Positioned NH Group as Positive Ionizable Moiety and Showing Neuroprotective Activity.
J Med Chem 67: 9150-9164 (0)
Welab Barcelona
Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.
J Med Chem 67: 9173-9193 (0)
University of Kentucky
Discovery of a Promising CBP/p300 Degrader XYD129 for the Treatment of Acute Myeloid Leukemia.
J Med Chem 67: 9194-9213 (0)
Shenyang Pharmaceutical University
Structure-Based Optimization of Novel Sterol 24-C-Methyltransferase Inhibitors for the Treatment of Candida albicans Infections.
J Med Chem 67: 9318-9341 (0)
Shandong University
Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders.
J Med Chem 67: 9355-9373 (0)
Intra-Cellular Therapies, Inc.
Discovery of the Selective and Orally Available Galectin-1 Inhibitor GB1908 as a Potential Treatment for Lung Cancer.
J Med Chem 67: 9374-9388 (0)
Galecto Biotech AB
Design, Synthesis, and Biological Evaluation of New 2,6,7-Substituted Purine Derivatives as Toll-like Receptor 7 Agonists for Intranasal Vaccine Adjuvants.
J Med Chem 67: 9389-9405 (0)
Gwangju Institute of Science and Technology
Hit-to-Lead Optimization of the Natural Product Oridonin as Novel NLRP3 Inflammasome Inhibitors with Potent Anti-Inflammation Activity.
J Med Chem 67: 9406-9430 (0)
China Pharmaceutical University
Structure-Based Design and Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High Selectivity, Brain Penetration, and In Vivo Efficacy.
J Med Chem 67: 9431-9446 (0)
Suzhou Genhouse Bio Co., Ltd.
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.
J Med Chem 67: 9447-9464 (0)
Wenzhou Medical University Lishui Hospital
Structure-Based Design of a Potent and Selective YTHDC1 Ligand.
J Med Chem 67: 9516-9535 (0)
University of Zurich
Systematic Structure-Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments.
J Med Chem 67: 9552-9574 (0)
Virginia Commonwealth University
Design, Synthesis, and Structure-Activity Relationships of Novel Peptide Derivatives of the Severe Acute Respiratory Syndrome-Coronavirus-2 Spike-Protein that Potently Inhibit Nicotinic Acetylcholine Receptors.
J Med Chem 67: 9587-9598 (0)
University of Utah
Development of Penicillin-Based Carbonic Anhydrase Inhibitors Targeting Multidrug-Resistant Neisseria gonorrhoeae.
J Med Chem 67: 9613-9627 (0)
University of Florence
Discovery of Novel Azaindoles as Potent and Selective PI3Kδ Inhibitors for Treatment of Multiple Sclerosis.
J Med Chem 67: 9628-9644 (0)
Zhejiang University
Discovery of 3-((4-Benzylpyridin-2-yl)amino)benzamides as Potent GPR52 G Protein-Biased Agonists.
J Med Chem 67: 9709-9730 (0)
University of Texas Medical Branch
Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure.
J Med Chem 67: 9731-9744 (0)
Bristol Myers Squibb
Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA.
J Med Chem 67: 9759-9771 (0)
Pfizer
Overcoming Secondary Mutations of Type II Kinase Inhibitors.
J Med Chem 67: 9776-9788 (0)
University of Arkansas
Discovery and Development of NLRP3 Inhibitors Targeting the LRR Domain to Disrupt NLRP3-NEK7 Interaction for the Treatment of Rheumatoid Arthritis.
J Med Chem 67: 9869-9895 (0)
China Pharmaceutical University
Potent, Selective Agonists for the Cannabinoid-like Orphan G Protein-Coupled Receptor GPR18: A Promising Drug Target for Cancer and Immunity.
J Med Chem 67: 9896-9926 (0)
University of Bonn
Advanced Design, Synthesis, and Evaluation of Highly Selective Wee1 Inhibitors: Enhancing Pharmacokinetics and Antitumor Efficacy.
J Med Chem 67: 9927-9949 (0)
China Pharmaceutical University
Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity.
J Med Chem 67: 10012-10024 (0)
Tampere University
Discovery of Orally Bioavailable and Potent CDK9 Inhibitors for Targeting Transcription Regulation in Triple-Negative Breast Cancer.
J Med Chem 67: 10035-10056 (0)
University of Chinese Academy of Sciences
Synthetically Feasible De Novo Molecular Design of Leads Based on a Reinforcement Learning Model: AI-Assisted Discovery of an Anti-IBD Lead Targeting CXCR4.
J Med Chem 67: 10057-10075 (0)
Hangzhou Normal University
Structure-Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD+-Dependent Lysine Deacylase Sirtuin 2.
J Med Chem 67: 10076-10095 (0)
University of Freiburg
Discovery and Optimization of Novel SaFabI Inhibitors as Specific Therapeutic Agents for MRSA Infection.
J Med Chem 67: 10096-10134 (0)
Sichuan University
Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine.
J Med Chem 67: 10135-10151 (0)
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
Identification and Validation of PKR as a Direct Target for the Novel Sulfonamide-Substituted Tetrahydroquinoline Nonselective Inhibitor of the NLRP3 Inflammasome.
J Med Chem 67: 10168-10189 (0)
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 1,2,4-Oxadiazole Derivatives Containing an Aryl Carboxylic Acid Moiety as Potent Sarbecovirus Papain-like Protease Inhibitors.
J Med Chem 67: 10211-10232 (0)
Peking Union Medical College and Chinese Academy of Medical Sciences
Discovery of N-Substituted Acetamide Derivatives as Promising P2Y14R Antagonists Using Molecular Hybridization Based on Crystallographic Overlay.
J Med Chem 67: 10233-10247 (0)
Children's Hospital Affiliated to Zhengzhou University
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
J Med Chem 67: 10248-10262 (0)
Pfizer
Discovery of a Novel ASM Direct Inhibitor with a 1,5-Diphenyl-pyrazole Scaffold and Its Antidepressant Mechanism of Action.
J Med Chem 67: 10350-10373 (0)
China Pharmaceutical University
Fentanyl-Type Antagonist of the μ-Opioid Receptor: Important Role of Axial Chirality in the Active Conformation.
J Med Chem 67: 10447-10463 (0)
Tokyo University of Science
Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.
J Med Chem 67: 10490-10507 (0)
Seoul National University
Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches.
J Med Chem 67: 10530-10547 (0)
Hebei University of Science & Technology
Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma.
J Med Chem 67: 10548-10566 (0)
Kymera Therapeutics
Development of a Potent and Selective G2A (GPR132) Agonist.
J Med Chem 67: 10567-10588 (0)
Fraunhofer Institute for Translational Medicine and Pharmacology ITMP
Discovery of Novel Proteolysis-Targeting Chimera Molecules as Degraders of Programmed Cell Death-Ligand 1 for Breast Cancer Therapy.
J Med Chem 67: 10589-10600 (0)
Sichuan University
G Protein-Coupled Estrogen Receptor-Mediated Anti-Inflammatory and Mucosal Healing Activity of a Trimethylpyridinol Analogue in Inflammatory Bowel Disease.
J Med Chem 67: 10601-10621 (0)
Yeungnam University
Discovery of 5-(Piperidin-4-yl)-1,2,4-oxadiazole Derivatives as a New Class of Human Caseinolytic Protease P Agonists for the Treatment of Hepatocellular Carcinoma.
J Med Chem 67: 10622-10642 (0)
Sichuan University
Discovery of Novel Receptor Tyrosine Kinase-like Orphan Receptor 1 (ROR1) Inhibitors for Cancer Treatment.
J Med Chem 67: 10655-10686 (0)
Sichuan University
Fragment-Based Anti-inflammatory Agent Design and Target Identification: Discovery of AF-45 as an IRAK4 Inhibitor to Treat Ulcerative Colitis and Acute Lung Injury.
J Med Chem 67: 10687-10709 (0)
Wenzhou Medical University
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis.
J Med Chem 67: 10710-10742 (0)
Julius-Maximilians-Universitat Wurzburg (JMU)
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma.
J Med Chem 67: 10743-10773 (0)
China Pharmaceutical University
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
J Med Chem 67: 10795-10830 (0)
University of Chinese Academy of Sciences
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
J Med Chem 67: 10831-10847 (0)
Pfizer
Discovery of GPR84 Fluorogenic Probes Based on a Novel Antagonist for GPR84 Bioimaging.
J Med Chem 67: 10875-10890 (0)
Chinese Academy of Sciences
Discovery of Dual MER/AXL Kinase Inhibitors as Bifunctional Small Molecules for Inhibiting Tumor Growth and Enhancing Tumor Immune Microenvironment.
J Med Chem 67: 10906-10927 (0)
National Health Research Institutes
Discovery of Highly Selective, Potent, Covalent, and Orally Bioavailable Factor XIIa Inhibitors for the Treatment of Thrombo-Inflammation.
J Med Chem 67: 10946-10966 (0)
Hefei University of Technology
Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation.
J Med Chem 67: 11103-11124 (0)
Chiesi Farmaceutici S.p.A
Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β-Glucocerebrosidase.
J Med Chem 67: 11168-11181 (0)
Astex Pharmaceuticals
Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1.
J Med Chem 67: 11209-11225 (0)
AstraZeneca
Discovery of JNJ-74856665: A Novel Isoquinolinone DHODH Inhibitor for the Treatment of AML.
J Med Chem 67: 11254-11272 (0)
Janssen Research and Development
Development of Degraders of Cyclin-Dependent Kinases 4 and 6 Based on Rational Drug Design.
J Med Chem 67: 11354-11364 (0)
East China Normal University
Design, Synthesis, and Activity Evaluation of Novel Benzazole Bifunctional Antifungal Inhibitors with an LDH Carrier.
J Med Chem 67: 11365-11388 (0)
Liaocheng University
Rational Molecular Editing: A New Paradigm in Drug Discovery.
J Med Chem 67: 11459-11466 (0)
Henan Normal University
New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives.
J Med Chem 67: 11488-11521 (0)
University of Bologna
New Strategies for Responding to SARS-CoV-2: The Present and Future of Dual-Target Drugs.
J Med Chem 67: 11522-11542 (0)
China Pharmaceutical University
ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights.
J Med Chem 67: 11597-11621 (0)
University of Lille
Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain.
J Med Chem 67: 11662-11687 (0)
Universite Paris Cite
NN1213 - A Potent, Long-Acting, and Selective Analog of Human Amylin.
J Med Chem 67: 11688-11700 (0)
Novo Nordisk A/S
Amphiphilic Heparinoids as Potent Antiviral Agents against SARS-CoV-2.
J Med Chem 67: 11885-11916 (0)
University of Queensland
Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy.
J Med Chem 67: 11917-11936 (0)
Nanjing University of Chinese Medicine
Structure-Guided Design of Potent Coronavirus Inhibitors with a 2-Pyrrolidone Scaffold: Biochemical, Crystallographic, and Virological Studies.
J Med Chem 67: 11937-11956 (0)
Wichita State University
Targeting Myeloperoxidase Ameliorates Gouty Arthritis: A Virtual Screening Success Story.
J Med Chem 67: 12012-12032 (0)
University of Sao Paulo
Electrophile Determines Cellular Phenotypes among XPO1-Targeting Small Molecules.
J Med Chem 67: 12033-12054 (0)
Case Western Reserve University
Discovery of Novel Diaryl-Substituted Fused Heterocycles Targeting Katanin and Tubulin with Potent Antitumor and Antimultidrug Resistance Efficacy.
J Med Chem 67: 12118-12142 (0)
Fudan University
Structure-Based Design and Discovery of a Potent and Cell-Active LC3A/B Covalent Inhibitor.
J Med Chem 67: 12184-12204 (0)
Fudan University
Lipid Trolling to Optimize A3 Adenosine Receptor-Positive Allosteric Modulators (PAMs).
J Med Chem 67: 12221-12247 (0)
National Institute of Diabetes and Digestive and Kidney Diseases
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
J Med Chem 67: 12261-12313 (0)
University of North Carolina at Chapel Hill
Molecular Transformers: Adaptive Multitarget Ligands for Esterase-Induced Transition from Analgesics to Anesthetics.
J Med Chem 67: 12349-12365 (0)
Sichuan University
Identification of 6-Anilino Imidazo[4,5-c]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers.
J Med Chem 67: 12366-12385 (0)
University of Auckland
Natural Product-Inspired Dopamine Receptor Ligands.
J Med Chem 67: 12463-12484 (0)
City University of New York
Discovery of Novel 1-Phenylpiperidine Urea-Containing Derivatives Inhibiting β-Catenin/BCL9 Interaction and Exerting Antitumor Efficacy through the Activation of Antigen Presentation of cDC1 Cells.
J Med Chem 67: 12485-12520 (0)
Anhui University of Chinese Medicine
Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors.
J Med Chem 67: 12534-12552 (0)
Goethe University
Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of Alzheimer's Disease.
J Med Chem 67: 12571-12600 (0)
Shenyang Pharmaceutical University
Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.
J Med Chem 67: 12632-12659 (0)
Johann Wolfgang Goethe-University
A Comprehensive In Vitro Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors.
J Med Chem 67: 12711-12734 (0)
University of Salerno
Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies.
J Med Chem 67: 12735-12759 (0)
Shanghai Institute of Materia Medica
Discovery of Novel Nonpeptidic and Noncovalent Small Molecule 3CLpro Inhibitors as anti-SARS-CoV-2 Drug Candidate.
J Med Chem 67: 12760-12783 (0)
University of Chinese Academy of Sciences
Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8.
J Med Chem 67: 12784-12806 (0)
University of Florida
Deuterium Editing of Small Molecules: A Case Study on Antitumor Activity of 1,4-Benzodiazepine-2,5-dione Derivatives.
J Med Chem 67: 12835-12854 (0)
Tsinghua University
Discovery of Novel Pyrimidine-Based Derivatives as Nav1.2 Inhibitors with Efficacy in Mouse Models of Epilepsy.
J Med Chem 67: 12912-12931 (0)
University of Chinese Academy of Sciences
The Development of a Highly Potent and Selective Human Toll-like Receptor 2 Agonist: Synthesis and Biological Evaluation of CaLGL-1 and Its Derivatives.
J Med Chem 67: 12932-12944 (0)
Lanzhou University
Discovery of GS-7682, a Novel 4'-Cyano-Modified C-Nucleoside Prodrug with Broad Activity against Pneumo- and Picornaviruses and Efficacy in RSV-Infected African Green Monkeys.
J Med Chem 67: 12945-12968 (0)
Gilead Sciences, Inc.
Rational In Silico Design of Selective TMPRSS6 Peptidomimetic Inhibitors via Exploitation of the S2 Subpocket.
J Med Chem 67: 12969-12983 (0)
Universite de Sherbrooke
New Class of Hsp90 C-Terminal Domain Inhibitors with Anti-tumor Properties against Triple-Negative Breast Cancer.
J Med Chem 67: 12984-13018 (0)
University of Ljubljana
Identification of the Clinical Candidate PF-07284890 (ARRY-461), a Highly Potent and Brain Penetrant BRAF Inhibitor for the Treatment of Cancer.
J Med Chem 67: 13019-13032 (0)
Enliven Therapeutics
Peptidic Boronic Acid Plasmodium falciparum SUB1 Inhibitors with Improved Selectivity over Human Proteasome.
J Med Chem 67: 13033-13055 (0)
The Francis Crick Institute
Discovery of Novel HDAC3 Inhibitors with PD-L1 Downregulating/Degrading and Antitumor Immune Effects.
J Med Chem 67: 13067-13088 (0)
Southern Medical University
Structural and Physicochemical Features of Oral PROTACs.
J Med Chem 67: 13106-13116 (0)
AstraZeneca
Hit-to-Lead Optimization of Heterocyclic Carbonyloxycarboximidamides as Selective Antagonists at Human Adenosine A3 Receptor.
J Med Chem 67: 13117-13146 (0)
University of Cambridge
Genomic Discovery and Structure-Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors.
J Med Chem 67: 13147-13173 (0)
LifeMine Therapeutics
Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer.
J Med Chem 67: 13271-13285 (0)
Shanghai Institute of Materia Medica
Design, Synthesis and Antitumor Activity of a Novel Class of SHP2 Allosteric Inhibitors with a Furanyl Amide-Based Scaffold.
J Med Chem 67: 13305-13323 (0)
Shandong University
Structural Optimization of Oxaprozin for Selective Inverse Nurr1 Agonism.
J Med Chem 67: 13324-13348 (0)
Ludwig-Maximilians-University of Munich
Design, Synthesis, and Evaluation of the Selective and Orally Active LSD1 Inhibitor with the Potential of Treating Heart Failure.
J Med Chem 67: 13409-13434 (0)
Zhengzhou University
Bipyridine Derivatives as NOP2/Sun RNA Methyltransferase 3 Inhibitors for the Treatment of Colorectal Cancer.
J Med Chem 67: 13446-13473 (0)
Zhejiang University
Discovery and Optimization of Hsp110 and sGC Dual-Target Regulators for the Treatment of Pulmonary Arterial Hypertension.
J Med Chem 67: 13474-13490 (0)
Central South University
Hydrazides as Inhibitors of Histone Deacetylases.
J Med Chem 67: 13512-13533 (0)
Universidade de Lisboa
Discovery of JAB-3312, a Potent SHP2 Allosteric Inhibitor for Cancer Treatment.
J Med Chem 67: 13534-13549 (0)
Jacobio Pharmaceuticals
A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
J Med Chem 67: 13550-13571 (0)
Pfizer
Exploring 2-Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story.
J Med Chem 67: 13572-13593 (0)
University of Southampton
Bioisosteres at C9 of 2-Deoxy-2,3-didehydro-N-acetyl Neuraminic Acid Identify Selective Inhibitors of NEU3.
J Med Chem 67: 13594-13603 (0)
University of Alberta
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
J Med Chem 67: 13604-13638 (0)
AstraZeneca
Identification and Characterization of a Blood-Brain Barrier Penetrant Inositol Hexakisphosphate Kinase (IP6K) Inhibitor.
J Med Chem 67: 13639-13665 (0)
Johns Hopkins School of Medicine
Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC).
J Med Chem 67: 13666-13680 (0)
Southern University of Science and Technology
Non-Covalent Inhibitors of SARS-CoV-2 Papain-Like Protease (PLpro): In Vitro and In Vivo Antiviral Activity.
J Med Chem 67: 13681-13702 (0)
University of Arizona
Discovery of Novel, Selective, and Nonbasic Agonists for the Kappa-Opioid Receptor Determined by Salvinorin A-Based Virtual Screening.
J Med Chem 67: 13788-13801 (0)
Freie Universitat Berlin
Discovery of Novel Azaphenothiazine Derivatives to Suppress Endometrial Cancer by Targeting GRP75 to Impair Its Interaction with IP3R and Mitochondrial Ca2+ Homeostasis.
J Med Chem 67: 13829-13851 (0)
East China University of Science and Technology
Discovery of an Exceptionally Orally Bioavailable and Potent HPK1 PROTAC with Enhancement of Antitumor Efficacy of Anti-PD-L1 Therapy.
J Med Chem 67: 13852-13878 (0)
Zhejiang University
Synthesis and Biological Evaluation of Pyrazole-Pyrimidones as a New Class of Correctors of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR).
J Med Chem 67: 13891-13908 (0)
University of Padova
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.
J Med Chem 67: 13925-13958 (0)
Shenyang Pharmaceutical University
Halogen Bonding Hot Spots as a Constraint in Virtual Screening: A Case Study of 5-HT7R.
J Med Chem 67: 14007-14015 (0)
Polish Academy of Sciences
Exploration of Hydrazide-Based HDAC8 PROTACs for the Treatment of Hematological Malignancies and Solid Tumors.
J Med Chem 67: 14016-14039 (0)
University of Groningen
Structure of Designer Antibody-like Peptides Binding to the Human C5a with Potential to Modulate the C5a Receptor Signaling.
J Med Chem 67: 14110-14124 (0)
Indian Institute of Technology Bhubaneswar
Discovery of CW-3308 as a Potent, Selective, and Orally Efficacious PROTAC Degrader of BRD9.
J Med Chem 67: 14125-14154 (0)
University of Michigan
Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione.
J Med Chem 67: 14184-14199 (0)
Bristol Myers Squibb
Accelerated Discovery of Carbamate Cbl-b Inhibitors Using Generative AI Models and Structure-Based Drug Design.
J Med Chem 67: 14210-14233 (0)
AstraZeneca
Synthesis and Biological Evaluation of Novel Psidium Meroterpenoid Derivatives against Cisplatin-Induced Acute Kidney Injury.
J Med Chem 67: 14234-14255 (0)
Peking Union Medical College
A First-in-Class Pyrazole-isoxazole Enhanced Antifungal Activity of Voriconazole: Synergy Studies in an Azole-Resistant Candida albicans Strain, Computational Investigation and in Vivo Validation in a Galleria mellonella Fungal Infection Model.
J Med Chem 67: 14256-14276 (0)
University of Naples Federico II
Discovery of 4-(Arylethynyl)piperidine Derivatives as Potent Nonsaccharide O-GlcNAcase Inhibitors for the Treatment of Alzheimer's Disease.
J Med Chem 67: 14292-14312 (0)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Novel Imidazo[1,2-a]pyridine-Based HDAC6 Inhibitors as an Anticarcinogen with a Cardioprotective Effect.
J Med Chem 67: 14345-14369 (0)
Zhengzhou University
Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors.
J Med Chem 67: 14370-14393 (0)
Vanderbilt University School of Medicine
Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M5 Muscarinic Acetylcholine Receptor.
J Med Chem 67: 14394-14413 (0)
Vanderbilt University
Development of Brain Penetrant Pyridazine Pantothenate Kinase Activators.
J Med Chem 67: 14432-14442 (0)
St. Jude Children's Research Hospital
Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy.
J Med Chem 67: 14443-14465 (0)
Gwangju Institute of Science and Technology
Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy.
J Med Chem 67: 14466-14477 (0)
Pfizer
Dual 5-HT2A and 5-HT2C Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis.
J Med Chem 67: 14478-14492 (0)
Shionogi Pharmaceutical Research Center
Property and Activity Refinement of Dihydroquinazolinone-3-carboxamides as Orally Efficacious Antimalarials that Target PfATP4.
J Med Chem 67: 14493-14523 (0)
The University of Melbourne
Domoic Acid as a Lead for the Discovery of the First Selective Ligand for Kainate Receptor Subtype 5 (GluK5).
J Med Chem 67: 14524-14542 (0)
University of Copenhagen
Structural Insights into Protein-Inhibitor Interactions in Human Tryptophan Dioxygenase.
J Med Chem 67: 14543-14552 (0)
Albert Einstein College of Medicine
Natural Derivatives of Selective HDAC8 Inhibitors with Potent in Vivo Antitumor Efficacy against Breast Cancer.
J Med Chem 67: 14609-14632 (0)
Zhejiang University
Discovering New Metallo-Deubiquitinase CSN5 Inhibitors by a Non-Catalytic Activity Assay Platform.
J Med Chem 67: 14649-14667 (0)
Sichuan University
Discovery of a Potent and Orally Bioavailable Xanthine Oxidase/Urate Transporter 1 Dual Inhibitor as a Potential Treatment for Hyperuricemia and Gout.
J Med Chem 67: 14668-14691 (0)
HEC Research and Development Center
Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies.
J Med Chem 67: 14702-14722 (0)
Jinan University
Cellular, Structural Basis, and Recent Progress for Targeting Murine Double Minute X (MDMX) in Tumors.
J Med Chem 67: 14723-14741 (0)
Yantai University
Small Molecular Inhibitors That Target ATM for Drug Discovery: Current Research and Potential Prospective.
J Med Chem 67: 14742-14767 (0)
Sichuan University
The Missing Link(er): A Roadmap to Macrocyclization in Drug Discovery.
J Med Chem 67: 14768-14785 (0)
Technical University of Darmstadt
Methyl-Transferase-Like Protein 16 (METTL16): The Intriguing Journey of a Key Epitranscriptomic Player Becoming an Emerging Biological Target.
J Med Chem 67: 14786-14806 (0)
University of Naples Federico II
Design and Evaluation of 3-Phenyloxetane Derivative Agonists of the Glucagon-Like Peptide-1 Receptor.
J Med Chem 67: 14820-14839 (0)
Huadong Medicine Company Limited
Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist for the Treatment of MASH.
J Med Chem 67: 14840-14851 (0)
Aligos Belgium BV
Evo312: An Evodiamine Analog and Novel PKCβI Inhibitor with Potent Antitumor Activity in Gemcitabine-Resistant Pancreatic Cancer.
J Med Chem 67: 14885-14911 (0)
Seoul National University
Targeting Relevant HDACs to Support the Survival of Cone Photoreceptors in Inherited Retinal Diseases: Identification of a Potent Pharmacological Tool with In Vitro and In Vivo Efficacy.
J Med Chem 67: 14946-14973 (0)
University of Siena
Nonpeptidic Irreversible Inhibitors of SARS-CoV-2 Main Protease with Potent Antiviral Activity.
J Med Chem 67: 14986-15011 (0)
University of Bonn
Nonlipogenic ABCA1 Inducers (NLAI) for Alzheimer's Disease Validated in a Mouse Model Expressing Human APOE3/APOE4.
J Med Chem 67: 15061-15079 (0)
University of Arizona
Allosteric Activation of Protein Phosphatase 5 with Small Molecules.
J Med Chem 67: 15080-15097 (0)
China Pharmaceutical University
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death.
J Med Chem 67: 15098-15117 (0)
Shandong University
Structure-Based Design and Development of Phosphine Oxides as a Novel Chemotype for Antibiotics that Dysregulate Bacterial ClpP Proteases.
J Med Chem 67: 15131-15147 (0)
University of Toronto
Exploring Degradation of Intrinsically Disordered Protein Yes-Associated Protein Induced by Proteolysis TArgeting Chimeras.
J Med Chem 67: 15168-15198 (0)
University of Florida
Discovery of Pyrazolo[1,5-a]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors.
J Med Chem 67: 15199-15219 (0)
Chinese Academy of Sciences
Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies.
J Med Chem 67: 15220-15245 (0)
University of Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of 5-Amino-4-fluoro-1H-benzo[d]imidazole-6-carboxamide Derivatives as Novel and Potential MEK/RAF Complex Inhibitors Based on the "Clamp" Strategy.
J Med Chem 67: 15246-15267 (0)
Sichuan University
Natural Product-Inspired Discovery of Naphthoquinone-Furo-Piperidine Derivatives as Novel STAT3 Inhibitors for the Treatment of Triple-Negative Breast Cancer.
J Med Chem 67: 15291-15310 (0)
Zhejiang University
Discovery of Dehydrogenated Imipridone Derivatives as Activators of Human Caseinolytic Protease P.
J Med Chem 67: 15328-15352 (0)
China Pharmaceutical University
Discovery of Covalent MLKL PROTAC Degraders via Optimization of a Theophylline Derivative Ligand for Treating Necroptosis.
J Med Chem 67: 15353-15372 (0)
China Pharmaceutical University
Rational Design of a Novel 6H-Benzo[c]chromen Series as Selective PI3Kα Inhibitors.
J Med Chem 67: 15387-15410 (0)
Xi'an Jiaotong University
A Mitochondria-Targeting SIRT3 Inhibitor with Activity against Diffuse Large B Cell Lymphoma.
J Med Chem 67: 15428-15437 (0)
Cornell University
Design, Synthesis, and Biological Activity of Novel Quinone Derivatives as Potent STAT3 Inhibitors for Psoriasis Treatment.
J Med Chem 67: 15438-15455 (0)
Central South University
Structural Optimization and Structure-Activity Relationship of 1H-Pyrazole-4-carboxylic Acid Derivatives as DNA 6mA Demethylase ALKBH1 Inhibitors and Their Antigastric Cancer Activity.
J Med Chem 67: 15456-15475 (0)
Sichuan University
Selective Aurora A-TPX2 Interaction Inhibitors Have In Vivo Efficacy as Targeted Antimitotic Agents.
J Med Chem 67: 15521-15536 (0)
University of Cambridge
Design, Synthesis, and Biological Evaluation of Potent EZH2/LSD1 Dual Inhibitors for Prostate Cancer.
J Med Chem 67: 15586-15605 (0)
Sun Yat-sen University Cancer Center
Design and Synthesis of 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylic Acid Derivatives as PP5 Inhibitors To Reverse Temozolomide Resistance in Glioblastoma Multiforme.
J Med Chem 67: 15691-15710 (0)
China Pharmaceutical University
Discovery of Potent, Specific, and Orally Available NLRP3 Inflammasome Inhibitors Based on Pyridazine Scaffolds for the Treatment of Septic Shock and Peritonitis.
J Med Chem 67: 15711-15737 (0)
Sichuan University
Discovery of Novel Neo-Clerodane Derivatives as Potent Dual-Functional Antiosteoporosis Agents through Targeting Peroxisome Proliferator-Activated Receptor-γ.
J Med Chem 67: 15738-15755 (0)
Sun Yat-sen University
Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs.
J Med Chem 67: 15780-15795 (0)
Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
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.
J Med Chem 67: 15816-15836 (0)
Jinan University
Structure-Activity Relationship Studies of Substituted 2-Phenyl-1,2,4-triazine-3,5(2H,4H)-dione Analogues: Development of Potent eEF2K Degraders against Triple-Negative Breast Cancer.
J Med Chem 67: 15837-15861 (0)
Soochow University
Investigating Active Site Binding of Ligands to High and Low Activity Carbonic Anhydrase Enzymes Using Native Mass Spectrometry.
J Med Chem 67: 15862-15872 (0)
Griffith University
Discovery of a Covalent Inhibitor of Pro-Caspase-1 Zymogen Blocking NLRP3 Inflammasome Activation and Pyroptosis.
J Med Chem 67: 15873-15891 (0)
Chinese Academy of Sciences
Harnessing Nitric Oxide-Donating Benzofuroxans for Targeted Inhibition of Carbonic Anhydrase IX in Cancer.
J Med Chem 67: 15892-15907 (0)
University of Florence
Structure, Function, and Activity of Small Molecule and Peptide Inhibitors of Protein Arginine Methyltransferase 1.
J Med Chem 67: 15931-15946 (0)
University of Manitoba
The "Doorstop Pocket" In Thioredoxin Reductases─An Unexpected Druggable Regulator of the Catalytic Machinery.
J Med Chem 67: 15947-15967 (0)
University of L'Aquila
Targeting HSP90 for Cancer Therapy: Current Progress and Emerging Prospects.
J Med Chem 67: 15968-15995 (0)
Sichuan University
Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential.
J Med Chem 67: 16018-16034 (0)
Shanghai Institute of Materia Medica
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.
J Med Chem 67: 16056-16071 (0)
Sun Yat-Sen University
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
J Med Chem 67: 16072-16087 (0)
Sun Yat-Sen University
Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension.
J Med Chem 67: 16128-16144 (0)
China Pharmaceutical University
Discovery of 2-Aryl-4-aminoquinazolin-Based LSD1 Inhibitors to Activate Immune Response in Gastric Cancer.
J Med Chem 67: 16165-16184 (0)
Zhengzhou University
Merging Natural Product Structures with Pharmaceutical Leads: Unnatural Enantiomers of Estranes as Glucocorticoid Receptor Modulators That Suppress TNF-α and IL-6 Release.
J Med Chem 67: 16185-16194 (0)
The Scripps Research Institute
Development of Nitric Oxide-Donating Netarsudil Derivatives as a Synergistic Therapy for Glaucoma with Reduced Ocular Irritation.
J Med Chem 67: 16311-16327 (0)
China Pharmaceutical University
Tuning RXR Modulators for PGC1α Recruitment.
J Med Chem 67: 16338-16354 (0)
Ludwig-Maximilians-Universitat (LMU) Munchen
Preclinical Evaluation of Dihydropyrazole-Cored Positron Emission Tomography (PET) Ligands for Imaging of Receptor-Interacting Serine/Threonine Protein Kinase 1 (RIPK1) in the Brain.
J Med Chem 67: 16403-16415 (0)
Beijing Normal University
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
J Med Chem 67: 16455-16479 (0)
AstraZeneca
Development of a First-in-Class DNMT1/HDAC Inhibitor with Improved Therapeutic Potential and Potentiated Antitumor Immunity.
J Med Chem 67: 16480-16504 (0)
Shandong University
Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Antialphavirus Activity.
J Med Chem 67: 16505-16532 (0)
University of North Carolina at Chapel Hill
Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases.
J Med Chem 67: 16533-16555 (0)
Institute of General Organic Chemistry (CSIC)
Structure-Activity Relationship of Inositol Thiophosphate Analogs as Allosteric Activators of Clostridioides difficile Toxin B.
J Med Chem 67: 16576-16597 (0)
McGill University
Development of Tailless Homologue Receptor (TLX) Agonist Chemical Tools.
J Med Chem 67: 16598-16611 (0)
Ludwig-Maximilians-Universitat (LMU) Munchen
Design, Synthesis, and Bioevaluation of Novel NLRP3 Inhibitor with IBD Immunotherapy from the Virtual Screen.
J Med Chem 67: 16612-16634 (0)
Fudan University
Inhibition of the EphA2-Sam/Ship2-Sam Association through Peptide Ligands: Studying the Combined Effect of Charge and Aromatic Character.
J Med Chem 67: 16649-16663 (0)
Institute of Biostructures and Bioimaging
Heat Shock Protein 90 Interactome-Mediated Proteolysis Targeting Chimera (HIM-PROTAC) Degrading Glutathione Peroxidase 4 to Trigger Ferroptosis.
J Med Chem 67: 16712-16736 (0)
Hangzhou Institute of Medicine (HIM)
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
J Med Chem 67: 16737-16756 (0)
Tyra Biosciences, Inc.
Discovery and Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors.
J Med Chem 67: 16807-16819 (0)
Merck & Co.
Enhanced Recognition Memory through Dual Modulation of Brain Carbonic Anhydrases and Cholinesterases.
J Med Chem 67: 16873-16898 (0)
University of Florence
A Lysosome-Targeting hNEU1 Inhibitor Treats Myocardial Infarction: A Potential Therapeutic Breakthrough.
J Med Chem 67: 16899-16911 (0)
Southeast University
An Adenosine Analogue Library Reveals Insights into Active Sites of Protein Arginine Methyltransferases and Enables the Discovery of a Selective PRMT4 Inhibitor.
J Med Chem 67: 18053-18069 (0)
Purdue University
Discovery of Imidazo[1,2-a]pyrazine Derivatives as Potent ENPP1 Inhibitors.
J Med Chem 67: 18317-18333 (0)
Shanghai Institute of Materia Medica
Discovery of Orally Active Phenylquinoline-Based Soluble Epoxide Hydrolase Inhibitors with Anti-Inflammatory and Analgesic Activity.
J Med Chem 67: 18412-18447 (0)
Beijing Institute of Technology
Discovery of Benzo[d]oxazoles as Novel Dual Small-Molecule Inhibitors Targeting PD-1/PD-L1 and VISTA Pathway.
J Med Chem 67: 18526-18548 (0)
China Pharmaceutical University