Journal of Medicinal Chemistry

Papers
(The H4-Index of Journal of Medicinal Chemistry is 68. 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 2021-06-01 to 2025-06-01.)
ArticleCitations
Issue Publication Information466
Issue Editorial Masthead432
Issue Editorial Masthead409
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate250
Macrocyclization as a Strategy for Kinetic Solubility Improvement: A Comparative Analysis of Matched Molecular Pairs236
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity221
Cyclodextrin-Activated Porphyrin Photosensitization for Boosting Self-Cleavable Drug Release199
Sertraline and Astemizole Enhance the Deubiquitinase Activity of USP7 by Binding to Its Switching Loop Region186
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr155
Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors153
Subtle Structural Changes across the Boundary between A2AR/A2BR Dual Antagonism and A2BR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives150
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I150
Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets147
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy134
Amino-Substituted 3-Aryl- and 3-Heteroarylquinolines as Potential Antileishmanial Agents128
ω-Functionalized Lipid Prodrugs of HIV NtRTI Tenofovir with Enhanced Pharmacokinetic Properties124
Diamino Allose Phosphates: Novel, Potent, and Highly Stable Toll-like Receptor 4 Agonists124
Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D3 (Calcitriol): Refinement of the Side Chain122
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma119
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor118
Diversity-Oriented A3-Macrocyclization for Studying Influences of Ring-Size and Shape of Cyclic Peptides: CD36 Receptor Modulators117
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach116
A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo111
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis110
Dynorphin Neuropeptides Decrease Apparent Proton Affinity of ASIC1a by Occluding the Acidic Pocket110
Multidisciplinary Training for Fostering Next-Generation Medicinal Chemists108
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery108
CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation106
Enhancing the Predictive Power of Machine Learning Models through a Chemical Space Complementary DEL Screening Strategy106
Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine106
Iterative Optimization and Structure–Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity103
Development of CD73 Inhibitors in Tumor Immunotherapy and Opportunities in Imaging and Combination Therapy101
All-d-Enantiomeric Peptide D3 Designed for Alzheimer’s Disease Treatment Dynamically Interacts with Membrane-Bound Amyloid-β Precursors101
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells100
Potent Lys Patch-Containing Stapled Peptides Targeting PCSK9100
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation99
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer99
Structure–Activity Relationships of Truncated 1′-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs97
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises95
Selection of QPX7831, an Orally Bioavailable Prodrug of Boronic Acid β-Lactamase Inhibitor QPX772894
Antibody-Vincristine Conjugates as Potent Anticancer Therapeutic Agents92
Structure–Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors91
Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations91
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor90
Potent, Selective, and Membrane Permeable 2-Amino-4-Substituted Pyridine-Based Neuronal Nitric Oxide Synthase Inhibitors89
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 R88
Antiviral Protein–Protein Interaction Inhibitors86
Navigating the Landscape of Academic Drug Discovery: An 18-Year Journey86
Crystallography-Guided Optimizations of the Keap1–Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides83
Rapid Response Antimicrobial Peptide Design Strategy Driven by Meta-Learning for Emerging Drug-Resistant Pathogens83
N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y4 Receptor Ligands Results in Picomolar Binding Constants82
Targeted Protein Degradation Induced by HEMTACs Based on HSP9080
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library78
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure−Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations78
Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series75
Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model75
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor75
Cell-Based Screen Identifies a Highly Potent and Orally Available ABCB1 Modulator for Treatment of Multidrug Resistance74
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir74
PEGylation of the Antimicrobial Peptide PG-1: A Link between Propensity for Nanostructuring and Capacity of the Antitrypsin Hydrolytic Ability72
Asymmetric Synthesis and Biological Screening of Quinoxaline-Containing Synthetic Lipoxin A4 Mimetics (QNX-sLXms)72
Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin αvβ6 Binding Peptide–Drug Conjugate for Tumor Targeted Drug Delivery72
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins72
Fused Cycloheptatriene–BODIPY Is a High-Performance Near-Infrared Probe to Image Tau Tangles72
Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor71
EP2 Antagonists (2011–2021): A Decade’s Journey from Discovery to Therapeutics71
Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with 9069
Progress on the Pharmacological Targeting of Janus Pseudokinases69
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit68
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