OOIR: Observatory of International Research

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.)

Article	Citations
Issue Publication Information	466
Issue Editorial Masthead	432
Issue Editorial Masthead	409
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate	250
Macrocyclization as a Strategy for Kinetic Solubility Improvement: A Comparative Analysis of Matched Molecular Pairs	236
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity	221
Cyclodextrin-Activated Porphyrin Photosensitization for Boosting Self-Cleavable Drug Release	199
Sertraline and Astemizole Enhance the Deubiquitinase Activity of USP7 by Binding to Its Switching Loop Region	186
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr	155
Design, Synthesis, and Biological Activity of Novel Ornithine Decarboxylase (ODC) Inhibitors	153
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	150
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I	150
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	147
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy	134
Amino-Substituted 3-Aryl- and 3-Heteroarylquinolines as Potential Antileishmanial Agents	128
Diamino Allose Phosphates: Novel, Potent, and Highly Stable Toll-like Receptor 4 Agonists	124
ω-Functionalized Lipid Prodrugs of HIV NtRTI Tenofovir with Enhanced Pharmacokinetic Properties	124
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	122
Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma	119
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor	118
Diversity-Oriented A³-Macrocyclization for Studying Influences of Ring-Size and Shape of Cyclic Peptides: CD36 Receptor Modulators	117
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach	116
A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo	111
Dynorphin Neuropeptides Decrease Apparent Proton Affinity of ASIC1a by Occluding the Acidic Pocket	110
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis	110

Multidisciplinary Training for Fostering Next-Generation Medicinal Chemists	108
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery	108
CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation	106
Enhancing the Predictive Power of Machine Learning Models through a Chemical Space Complementary DEL Screening Strategy	106
Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine	106
Iterative Optimization and Structure–Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity	103
Development of CD73 Inhibitors in Tumor Immunotherapy and Opportunities in Imaging and Combination Therapy	101
All-d-Enantiomeric Peptide D3 Designed for Alzheimer’s Disease Treatment Dynamically Interacts with Membrane-Bound Amyloid-β Precursors	101
A Novel Anticancer Stem Cell Compound Derived from Pleuromutilin Induced Necroptosis of Melanoma Cells	100
Potent Lys Patch-Containing Stapled Peptides Targeting PCSK9	100
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation	99
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer	99
Structure–Activity Relationships of Truncated 1′-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs	97
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises	95
Selection of QPX7831, an Orally Bioavailable Prodrug of Boronic Acid β-Lactamase Inhibitor QPX7728	94
Antibody-Vincristine Conjugates as Potent Anticancer Therapeutic Agents	92
Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations	91
Structure–Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors	91
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor	90
Potent, Selective, and Membrane Permeable 2-Amino-4-Substituted Pyridine-Based Neuronal Nitric Oxide Synthase Inhibitors	89
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	88
Navigating the Landscape of Academic Drug Discovery: An 18-Year Journey	86
Antiviral Protein–Protein Interaction Inhibitors	86
Crystallography-Guided Optimizations of the Keap1–Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides	83
Rapid Response Antimicrobial Peptide Design Strategy Driven by Meta-Learning for Emerging Drug-Resistant Pathogens	83
N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y₄ Receptor Ligands Results in Picomolar Binding Constants	82
Targeted Protein Degradation Induced by HEMTACs Based on HSP90	80
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure−Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations	78
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library	78
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A_2A Adenosine Receptor	75
Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series	75
Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model	75
Cell-Based Screen Identifies a Highly Potent and Orally Available ABCB1 Modulator for Treatment of Multidrug Resistance	74
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir	74
PEGylation of the Antimicrobial Peptide PG-1: A Link between Propensity for Nanostructuring and Capacity of the Antitrypsin Hydrolytic Ability	72
Asymmetric Synthesis and Biological Screening of Quinoxaline-Containing Synthetic Lipoxin A₄ Mimetics (QNX-sLXms)	72
Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin α_vβ₆ Binding Peptide–Drug Conjugate for Tumor Targeted Drug Delivery	72
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins	72
Fused Cycloheptatriene–BODIPY Is a High-Performance Near-Infrared Probe to Image Tau Tangles	72
Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor	71
EP2 Antagonists (2011–2021): A Decade’s Journey from Discovery to Therapeutics	71
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 ⁹⁰	69
Progress on the Pharmacological Targeting of Janus Pseudokinases	69
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit	68