OOIR: Observatory of International Research

Papers

(The TQCC of Journal of Medicinal Chemistry is 14. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2022-06-01 to 2026-06-01.)

Article	Citations
pH-Responsive Self-Assembled Upconversion Photosensitizer and RSL3 Synergistically Induce Tumor Ferroptosis	766
Unmasking Conformationally Adaptable Lipids as Drug Receptors	402
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I	268
Issue Editorial Masthead	231
Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model	198
Turning the Spotlight Away from PDT: Chemodynamic Dominance of 2-(2-Bromopyridin-4-yl)-1 H -imidazo[4,5- f	192
Discovery of Cdc20/Hsp90 Dual-Target Inhibitors with Potent Antitumor Activity for Therapy of Acquired Resistant Melanoma	164
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy	163
Optimization of 2,8-Diaryl-1,5-naphthyridines as Plasmodium falciparum Phosphatidylinositol 4-Kinase Inhibitors with Improved ADME Profiles and In Vivo E	163
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis	162
Multidisciplinary Training for Fostering Next-Generation Medicinal Chemists	149
A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo	144
Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor	140
Probing Guanidino Pendant or Bridged Groups in Cyclic Antimicrobial Peptides Derived from Temporin L: A Strategy to Improve Efficacy against Gram-Negative Bacteria	131
Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”	126
Discovery of the First-In-Class HSD17B13/PPAR Multitarget Modulators for the Treatment of Metabolic Dysfunction-Associated Steatohepatitis	124
Navigating the Landscape of Academic Drug Discovery: An 18-Year Journey	124
Toward Dose Prediction at Point of Design	122
Therapeutic Potential of Novel Antimicrobial Peptide Pap12-6-10: Mechanisms of Antibacterial and Anti-inflammatory Action Against Gram-Negative Sepsis	119
Targeting Toll-like Receptors 7, 8, and 9 Inhibition in Systemic Lupus Erythematosus: Therapeutic Advance and Future Directions	119
Accurate Prediction of Core-Hopping Transformations Using Molecular Dynamics-Derived Conformational Ensembles: Application to the Discovery of Novel P2X3 Antagonists	112
AKR1C3 Inhibition: A Strategy to Reverse Osimertinib Resistance in Non-small Cell Lung Cancer	109
Antiviral Protein–Protein Interaction Inhibitors	104
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 R	102
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A_2A Adenosine Receptor	102

Discovery of YFJ-36: Design, Synthesis, and Antibacterial Activities of Catechol-Conjugated β-Lactams against Gram-Negative Bacteria	102
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library	100
Antibody-Vincristine Conjugates as Potent Anticancer Therapeutic Agents	93
Structure–Activity Relationship Guided Scaffold Hopping Resulted in the Identification of GLPG4970, a Highly Potent Dual SIK2/SIK3 Inhibitor	93
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)	90
Fragment-Based Development of Small Molecule Inhibitors Targeting Mycobacterium tuberculosis Cholesterol Metabolism	90
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins	89
Progress on the Pharmacological Targeting of Janus Pseudokinases	89
Sertraline and Astemizole Enhance the Deubiquitinase Activity of USP7 by Binding to Its Switching Loop Region	88
Discovery of Furan-2-Carboxylic Acid Derivatives as Novel D-Dopachrome Tautomerase (D-DT) and Macrophage Migration Inhibitory Factor-1 (MIF-1) Dual Inhibitors	88
Subtle Structural Changes across the Boundary between A_2AR/A_2BR Dual Antagonism and A_2BR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives	88
Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic	88
Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1	86
Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2	85
Carboxylesterase-Triggered Theranostic Agent: Advancing Near-Infrared Imaging and Therapeutic Efficacy in Hepatocellular Carcinoma	83
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr	82
Discovery of 2-(Pyrazol-4-yl)-quinazolin-4(3H)-one Derivatives as Subnanomolar BRD4 BD2 Inhibitors with High Selectivity via a Bioisosterism Approach	81
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer	81
Discovery of a Highly Potent and Selective Small-Molecule Inhibitor of In Vivo Anaerobic Choline Metabolism by Human Gut Bacteria	80
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery	80
Design and Synthesis of PARP/CDK6 Dual-Target Inhibitors Modulating of Wnt/β-Catenin Signaling Pathway for the Treatment of BRCA Wild-Type TNBC	77
Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation	77
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma	77
N-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia	76
Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series	76
How a Medicinal Chemistry Project Changed the Way Prostate Cancer is Diagnosed and Treated	75
Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment	74
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity	74
The New Frontier: Merging Molecular Glue Degrader and Antibody–Drug Conjugate Modalities To Overcome Strategic Challenges	73
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists	73
Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput	71
Diamino Allose Phosphates: Novel, Potent, and Highly Stable Toll-like Receptor 4 Agonists	71
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure−Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations	71
Rezatapopt (PC14586): A First-in-Class Small Molecule p53 Y220C Mutant Protein Stabilizer in Clinical Trials	71
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor	70
Micromonospora: A Prolific Source of Bioactive Secondary Metabolites with Therapeutic Potential	70
Small Molecule Inhibitors Targeting the “Undruggable” Survivin: The Past, Present, and Future from a Medicinal Chemist’s Perspective	70
Discovery of RP-1664: A First-in-Class Orally Bioavailable, Selective PLK4 Inhibitor	70
Rational Design of Schiff Base Copper Chelators as Potent Necroptosis Inducers for Anticancer Therapy	69
Spacial Score─A Comprehensive Topological Indicator for Small-Molecule Complexity	69
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises	69
Identification of Non-competitive and Reversible Inhibitors of Glycine Transporter 2: A Promising Non-opioid Therapeutic Strategy for Neuropathic Pain	69
Rapid Response Antimicrobial Peptide Design Strategy Driven by Meta-Learning for Emerging Drug-Resistant Pathogens	69
Optimization of Chelator Conjugation to PD-1/VEGF Bispecific Antibody for ⁸⁹ Zr-ImmunoPET Imaging	69
Cell-Based Screen Identifies a Highly Potent and Orally Available ABCB1 Modulator for Treatment of Multidrug Resistance	68
Molecular Skeleton Editing for New Drug Discovery	67
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation	67
Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis	67
Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-κB Ligand	67
Iterative Optimization and Structure–Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity	66

Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer	65
Discovery of Histone Deacetylase 8-Specific Proteolysis-Targeting Chimeras with Anticancer Activity against Hematological Malignancies	65
Development of CD73 Inhibitors in Tumor Immunotherapy and Opportunities in Imaging and Combination Therapy	65
Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8	64
Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation	64
In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel	63
Macrocyclic Neutralizer to Polybrene via Direct Host–Guest Complexation	63
Identification of Potent, Broad-Spectrum Coronavirus Main Protease Inhibitors for Pandemic Preparedness	63
Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation	63
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer	63
Macrocyclization as a Strategy for Kinetic Solubility Improvement: A Comparative Analysis of Matched Molecular Pairs	62
Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy	62
Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine	62
Structure–Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors	62
Discovery of Covalent MLKL PROTAC Degraders via Optimization of a Theophylline Derivative Ligand for Treating Necroptosis	62
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib	61
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1	61
Design of a Fluorescence Polarization Probe for Enterovirus 2C Proteins	60
Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets	60
Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders	60
Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors	60
Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives	59
Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin α_vβ₆ Binding Peptide–Drug Conjugate for Tumor Targeted Drug Delivery	59
Crystallography-Guided Optimizations of the Keap1–Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides	59
Fused Cycloheptatriene–BODIPY Is a High-Performance Near-Infrared Probe to Image Tau Tangles	58
From KRAS ^G12D to Pan-KRAS Inhibitors─A Journey Enabled by Synthetic Innovation and Structure-Base	58
Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors	58
Computational Screening of Phytocompounds Isolated from Clitoria ternatea Targeting the Inflammatory Pathway: Isoquercetin Identified as an IκB Kinase β	58
Discovery of MKP10241, a Novel Small Molecule Targeting the GPR119/Incretin Axis to Treat Metabolic Disorders	58
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach	57
Potent Zinc(II)-Based Immunogenic Cell Death Inducer Triggered by ROS-Mediated ERS and Mitochondrial Ca²⁺ Overload	57
Potent, Selective, and Membrane Permeable 2-Amino-4-Substituted Pyridine-Based Neuronal Nitric Oxide Synthase Inhibitors	56
Revitalizing PI3K Inhibitors for PET/CT Imaging and Radionuclide Therapy of Multiple Cancers	56
⁸⁹ Zr/ ¹⁷⁷ Lu-Labeled Radioimmunoconjugates Targeting SORT1 for Cancer Theranostics	56
Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches	55
Enhancing the Predictive Power of Machine Learning Models through a Chemical Space Complementary DEL Screening Strategy	55
Correction to “Nitroimidazole Containing [ ⁶⁸ Ga]Ga-IPM-N001 as a New CAIX-Targeting Radionuclide Tracer”	54
Rational Design of Broad-Spectrum Non-Nucleoside Reverse Transcriptase Inhibitors via Pharmacophore-Oriented Generative Artificial Intelligence	54
Design, Synthesis, and Evaluation of Indolizine Derivatives as Nonclassical Ferroptosis Inhibitors with Efficacy in Acute Liver Injury and Ischemic Stroke Models	54
Multivalent Peptide-Guided EZH2 Degradation Sensitizes Immune Checkpoint Therapy in TNBC	54
Identification of VVD-214/RO7589831, a Clinical-Stage, Covalent Allosteric Inhibitor of WRN Helicase for the Treatment of MSI-High Cancers	54
Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D₃ (Calcitriol): Refinement of the Side Chain	54
Issue Publication Information	54
Structure-Based Optimization of Pyridone α-Ketoamides as Inhibitors of the SARS-CoV-2 Main Protease	54
Structure–Activity Relationships of Truncated 1′-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs	53
Discovery of 3-(Fluoro-imidazolyl)pyridazine Derivatives as Potent STING Agonists with Antitumor Activity	53
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor	53
Efficacy, Mechanism, and Structure–Activity Relationship of 6-Methoxy Benzofuran Derivatives as a Useful Tool for Senile Osteoporosis	53
Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities	53
Occurrence of “Natural Selection” in Successful Small Molecule Drug Discovery	52
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 Validati	52
Mechanism of CRM1 Inhibition by Lansoprazole and Its Synergy with Cisplatin in Gastric Cancer	52
Discovery of Ruthenium(II) Metallocompound and Olaparib Synergy for Cancer Combination Therapy	52
NSAID–Au(I) Complexes Induce ROS-Driven DAMPs and Interpose Inflammation to Stimulate the Immune Response against Ovarian Cancer	52
Darizmetinib (HRX215): A Promising 1st-in-Class Liver Regenerating Drug in Phase 1b/2a Clinical Development, Targeting the Stress Signaling Protein Kinase MKK4	52
Pyrazolone-Based Zn(II) Complexes Display Antitumor Effects in Mutant p53-Carrying Cancer Cells	52
Real-Time NanoBRET Target Engagement Reveals Permeability-Activity Relationships in BET-Targeting Degraders	52
Heparan Sulfate-Based Neoproteoglycan for Targeted Lysosomal Degradation of Amyloid-β	51
Discovery of the Clinical Candidate S-892216 : A Second-Generation of SARS-CoV-2 3CL Protease Inhibitor for Treating COVID-19	51
Targeted Protein Degradation Induced by HEMTACs Based on HSP90	51
Discovery of Juglone Derivatives as Novel STAT3 Inhibitors with Potent Suppression of Cancer Cell Stemness against Breast Cancer	51
Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations	50
Discovery of a Potent, Selective and In Vivo Active Aurora A PROTAC Degrader from a Promiscuous Kinase Inhibitor	50
The Role of Allylic Strain for Conformational Control in Medicinal Chemistry	50
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir	49
Discovery of Highly Selective CYP1B1 Inhibitors	49
Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease	49
A New Era of Artificial Intelligence (AI): Transforming Drug Discovery and Development	49
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury	49
Call for Papers: Peptide Therapeutics	48
Harnessing Chimeric Degrader Technologies for Antimicrobial Innovation	48
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390	48
Discovery of Novel Antiepileptic Agents Targeting the α1β2γ2 GABA_A Receptor	48
Discovery of Novel 11-Membered Templates as Squalene Synthase Inhibitors	48
Mannich Base PIP-199 Is a Chemically Unstable Pan-Assay Interference Compound	48
Self-Assembly versus Coassembly: An Amphiphilic NIR-II Aggregation-Induced Emission Luminogen for Phototheranostics of Orthotopic Glioblastoma	48
α-Aminoboronic Acid Moieties in Boro Dipeptides Modulate Proteasome Subunit Selectivity and Provide Access to Compounds with Potent Anticancer and Anti-Inflammatory Activity	48
Design, Synthesis, and Characterization of Dichlorobiphenyl-Derived Inhibitors of the Proprotein Convertase Furin	48
Design, Synthesis, and Biological Evaluation of 2-Hydroxy-4-phenylthiophene-3-carbonitrile as PD-L1 Antagonist and Its Comparison to Available Small Molecular PD-L1 Inhibitors	48
ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases	47

In Silico-Guided Discovery and In Vitro Evaluation of Natural Sortase A Inhibitors to Fight Multidrug-Resistant Staphylococcus aureus	47
Correction to “Discovery of Novel Histone Deacetylase 6 (HDAC6) Inhibitors with Enhanced Antitumor Immunity of Anti-PD-L1 Immunotherapy in Melanoma”	47
Discovery of Potent, Selective, and Orally Bioavailable DYRK2 Inhibitors for the Treatment of Prostate Cancer	47
Novel 2-(2-Thienyl)-thiazolo[4,5-d]pyrimidin-7(6H)-ones Binding β+/α– Subunit Interface as GABA_AR Positive Allosteric Modulator for the Treatment of Status Epilepticus in Mous	47
Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14	46
Investigating Active Site Binding of Ligands to High and Low Activity Carbonic Anhydrase Enzymes Using Native Mass Spectrometry	46
Design, Synthesis, and Bioevaluation of a Novel Hybrid Molecular Pyrrolobenzodiazepine–Anthracenecarboxyimide as a Payload for Antibody–Drug Conjugate	46
Polarity-Tuned Lipid Droplet-Specific Probe for Heart Failure Imaging	46
Beyond the “2 + 2 Pharmacophore” Electronic and Hydrophobic Effects Control the Activity of Cationic Amphiphilic Antimicrobial 2,5-Diketopiperazines	46
Addressing the Intracellular Vestibule of the Plasmodial Lactate Transporter PfFNT by p-Substituted Inhibitors Amplifies In Vitro Activity	46
Cheminformatic Analysis of Core-Atom Transformations in Pharmaceutically Relevant Heteroaromatics	46
Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents	46
Pyrazolo-Pyrimidinones with Improved Solubility and Selective Inhibition of Adenylyl Cyclase Type 1 Activity for Treatment of Inflammatory Pain	46
Correction to “Design, Synthesis, and Evaluation of the Selective and Orally Active LSD1 Inhibitor with the Potential of Treating Heart Failure”	46
Inhibition of Wnt Signaling Using Axin Peptidomimetics through Direct Targeting of β-Catenin	45
Discovery of Orally Available Prodrugs of Itaconate and Derivatives	45
Chemical Space Navigation of Nitidine Leads to the Discovery of a Novel PD-L1 Degradation Agent by Targeting CSN5 for Enhanced Antitumor Immunity	45
Developing an Anticancer Platinum(II) Compound Based on the Uniqueness of Human Serum Albumin	45
Development of a High-Efficacy and Low-Toxicity Cobalt(II) Agent for Targeting Inhibition of Tumor Growth through Mitochondrial Damage-Mediated Chemotherapy and Immunotherapy	45
Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders	45
Discovery of Novel Azaphenothiazine Derivatives to Suppress Endometrial Cancer by Targeting GRP75 to Impair Its Interaction with IP3R and Mitochondrial Ca²⁺ Homeostasis	45
A Novel PSMA/FAP-Specific Radiotracer ^99mTc-HFaPSMA for Diagnosis of PSMA-Negative Prostate Cancer: From Preclinical Validation to Clinical Translation	44
The Discovery of RGH-706, a Highly Efficacious MCH1 Receptor Antagonist, for the Treatment of Obesity and Insatiable Hunger	44
Proposed Cuts to Health Research Threaten the Future of Drug Discovery and Development	44
Designing an Osmium(II) Complex to Inhibit the Growth and Recurrence of Tumors by Integrating Photodynamic Therapy, Chemotherapy, and Immunotherapy	44
Correction to “A NIR-II Photoacoustic/NIR-IIa Fluorescent Probe for Targeted Imaging of Glioma under NIR-II Excitation”	44
Identification of DC-174 as a Novel Hydroxamic Precandidate for the Development of an Oral Snakebite Treatment	44
Discovery of 2-Amino-7-sulfonyl-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluat	43
Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington’s Disease	43
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors	43
Discovery of Novel Potent Molecule for Treating Cisplatin-Induced Acute Kidney Injury Driven by Phenotypic Screening	43
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe	43
Structure-Based Design and Discovery of a Potent and Cell-Active LC3A/B Covalent Inhibitor	43
A Multi-Channel Machine Learning Model for Predicting the Bioactivity Potential of Macrocyclic Peptides	43
Discovery and Optimization of Tambjamines as a Novel Class of Antileishmanial Agents	43
Discovery of Potent and Selective Pyrrolo[2,3-d]Pyrimidine-Based Aurora A Inhibitors with Demonstrated Efficacy against Patient-Derived Gastric Cancer Organoids	43
Potent Long-Acting Inhibitors Targeting the HIV-1 Capsid Based on a Versatile Quinazolin-4-one Scaffold	42
A Medicinal Chemistry Perspective on Excitatory Amino Acid Transporter 2 Dysfunction in Neurodegenerative Diseases	42
Development and Discovery of a Selective Degrader of Casein Kinases 1 δ/ε	42
Combination of DNA Damage, Autophagy, and ERK Inhibition: Novel Evodiamine-Inspired Multi-Action Pt(IV) Prodrugs with High-Efficiency and Low-Toxicity Antitumor Activity	42
Discovery of Nelutroctiv (CK-136), a Selective Cardiac Troponin Activator for the Treatment of Cardiovascular Diseases Associated with Reduced Cardiac Contractility	42
Structure-Guided Discovery of Selective USP7 Inhibitors with In Vivo Activity	42
Discovery of Potent and Selective PI3Kδ Inhibitors for the Treatment of Acute Myeloid Leukemia	42
Discovery of Potent and Brain-Penetrant Bicyclic NLRP3 Inhibitors with Peripheral and Central In Vivo Activity	41
Elucidating Binding Selectivity in Cyclin-Dependent Kinases 4, 6, and 9: Development of Highly Potent and Selective CDK4/9 Inhibitors	41
N -Aryl- N -Lactosylamides as Potent and Highly Selective Inhibitors of Galectin-3 with Antifibrotic Activity	41
Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization	41
Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4	41
Recent Progress toward the Discovery of Small Molecules as Novel Anti-Respiratory Syncytial Virus Agents	41
Discovery and Characterization of GLPG3808, a PAPD5/7 Inhibitor for Suppression of Hepatitis B Viral Infections	41
Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov)	41
Rational Design and Synthesis of Highly Stable Haloflavanone DNA Methyltransferase Inhibitors Inducing Tumor Suppressor Gene Re-expression in Cancer Cells	41
HBsAg Suppression by a New Series of HBV RNA Destabilizers: Discovery and Effects on In Vitro Neurite Outgrowth	41
Impact of Fluorine Pattern on Lipophilicity and Acid–Base Properties of 2-(Thiofluoroalkyl)pyridines: Insights from Experiments and Statistical Modeling	40
A DNA-Mediated Lysosomal Degradation Strategy for Targeted Degradation of PD-L1 Protein	40
Developing Novel Coumarin-Containing Azoles Antifungal Agents by the Scaffold Merging Strategy for Treating Azole-Resistant Candidiasis	40
Design and Evaluation of Novel Ginger 6-Shogaol-Inspired Phospholipase C Inhibitors to Enhance β-Agonist-Induced Relaxation in Human Airway Smooth Muscle	40
[⁶⁸Ga]Ga-Ornibactin for Burkholderia cepacia complex Infection Imaging Using Positron Emission Tomography	40
Development of Fluorescent AF64394 Analogues Enables Real-Time Binding Studies for the Orphan Class A GPCR GPR3	40
Engineered Nanobody Chimeras Recruits Anti-HBV Antibodies for Target Cancer Immunotherapy	40
Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7	40
Discovery of a Novel MNK Inhibitor (NSP-1047) with In Vivo Anti-acute Myeloid Leukemia Activity	40
Discovery of NLX-266, an Orally Available and Metabolically Stable ERK1/2-Biased 5-HT_1AR Agonist with Superior Antidepressant and Antiparkinsonian Activity	40
Structure–Activity Relationships of Bis-Intercalating Peptides and Their Application as Antibody–Drug Conjugate Payloads	40
Structure-Based Discovery of High-Affinity Small Molecule Ligands and Development of Tool Probes to Study the Role of Chitinase-3-Like Protein 1	40
Development of a Chemical Probe to Enable Characterization of the Casein Kinase 1γ Subfamily	40
Structure–Activity Relationships of Natural and Semisynthetic Plecomacrolides Suggest Distinct Pathways for HIV-1 Immune Evasion and Vacuolar ATPase-Dependent Lysosomal Acidification	40
ARE-PROTACs Enable Co-degradation of an Nrf2–MafG Heterodimer	39
Discovery of Novel PROTAC SIRT6 Degraders with Potent Efficacy against Hepatocellular Carcinoma	39
A New Gramicidin S Analogue with Potent Antibacterial Activity and Negligible Hemolytic Toxicity	39
MTA-Cooperative PRMT5 Inhibitors: Mechanism Switching Through Structure-Based Design	39
New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives	39
Correction to “SH2 scan : Mapping SH2 Domain-Ligand Binding Selectivity for Inhibitors and Degraders”	39
Discovery of a Mixed and Prodrug-Like Inhibition Mechanism for Phosphocoumarins and Phosphoquinolinones against Human Carbonic Anhydrases	39
Synthesis of Heterocyclic Ring-Fused Bisnoralcohol Derivatives as Novel Small-Molecule Antiosteoporosis Agents	39
Tuning the Metabolic Stability of Visual Cycle Modulators through Modification of an RPE65 Recognition Motif	39
Development of PRC1 Inhibitors Employing Fragment-Based Approach and NMR-Guided Optimization	39
Pyridinophane Ligands: An Attractive Chelator Platform for Mn-Based Imaging Agents	39
Drug Discovery in Poland and Ukraine	39
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors	38
Linker-Driven Breakthrough: Design of a Novel Linker for Enhanced Theranostic Performance of FAPI Trimer	38
On-DNA Binder Confirmation: Increasing Confidence in DEL Hits	38
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2	38
Design of Proteolytic-Resistant Antifungal Peptides by Utilizing Minimum d-Amino Acid Ratios	38
Rationally Designed Highly Potent NKT Cell Agonists with Different Cytokine Selectivity through Hydrogen-Bond Interaction	38
Targeting KRAS Diversity: Covalent Modulation of G12X and Beyond in Cancer Therapy	38
Deubiquitinase-Targeting Chimeras (DUBTACs) as a Potential Paradigm-Shifting Drug Discovery Approach	38
Allosteric Activation of Protein Phosphatase 5 with Small Molecules	38
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones	37
Lead Optimization of Butyrolactone I as an Orally Bioavailable Antiallergic Agent Targeting FcγRIIB	37
Fluorescent Marinoquinoline Derivative as Inhibitors of Plasmodium falciparum : SAR Analysis, Mode of Action and In Vivo Studies	37
Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T-Cell Acute Lymphoblastic Leukemia	37
Benzoic Acid Derivatives Improve Plasma Stability of Diester Butyrophilin Ligand Prodrugs	37
Discovery of Novel N-Hydroxy-1,2,4-oxadiazole-5-formamides as ASM Direct Inhibitors for the Treatment of Atherosclerosis	37
Mapping the Lipid Signatures in COVID-19 Infection: Diagnostic and Therapeutic Solutions	37