OOIR: Observatory of International Research

Papers

(The H4-Index of Journal of Medicinal Chemistry is 69. 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 2020-11-01 to 2024-11-01.)

Article	Citations
U.S. FDA Approved Drugs from 2015–June 2020: A Perspective	402
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS^G12D Inhibitor	334
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19	326
Spirocyclic Scaffolds in Medicinal Chemistry	304
Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design	249
Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery	182
A Decade of FDA-Approved Drugs (2010–2019): Trends and Future Directions	168
Rings in Clinical Trials and Drugs: Present and Future	159
Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities	152
Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis	144
Decision Making in Structure-Based Drug Discovery: Visual Inspection of Docking Results	138
Incorporating Selenium into Heterocycles and Natural Products─From Chemical Properties to Pharmacological Activities	136
Peptide–Drug Conjugates with Different Linkers for Cancer Therapy	132
Reactive Oxygen Species (ROS)-Responsive Prodrugs, Probes, and Theranostic Prodrugs: Applications in the ROS-Related Diseases	125
Design of SARS-CoV-2 PLpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity	123
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors	114
Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation	112
InteractionGraphNet: A Novel and Efficient Deep Graph Representation Learning Framework for Accurate Protein–Ligand Interaction Predictions	111
Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras	110
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy	107
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP	106
Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy	97
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer	96
Critical Analysis of Drug Product Recalls due to Nitrosamine Impurities	96
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties	95

Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer	94
Strategies for Structural Modification of Small Molecules to Improve Blood–Brain Barrier Penetration: A Recent Perspective	91
Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease	89
Generative Models for De Novo Drug Design	89
Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer	88
Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL^pro)	87
Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative	87
3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents	86
Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development	85
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer	83
On the Frustration to Predict Binding Affinities from Protein–Ligand Structures with Deep Neural Networks	83
Has Ferrocene Really Delivered Its Role in Accentuating the Bioactivity of Organic Scaffolds?	82
Phenols in Pharmaceuticals: Analysis of a Recurring Motif	82
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity	82
Recent Progress on Tubulin Inhibitors with Dual Targeting Capabilities for Cancer Therapy	81
Membrane-Targeting Neolignan-Antimicrobial Peptide Mimic Conjugates to Combat Methicillin-Resistant Staphylococcus aureus (MRSA) Infections	81
Strategies for Targeting the NLRP3 Inflammasome in the Clinical and Preclinical Space	80
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models	80
Recent Update on Targeting c-MYC G-Quadruplexes by Small Molecules for Anticancer Therapeutics	79
CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia	79
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2	78
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors	78
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer’s Disease	78
The Ascension of Targeted Covalent Inhibitors	78
1,4,9-Triazaspiro[5.5]undecan-2-one Derivatives as Potent and Selective METTL3 Inhibitors	77
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir	77
Tuberculosis Drug Discovery: Challenges and New Horizons	76
Rational Multitargeted Drug Design Strategy from the Perspective of a Medicinal Chemist	75
Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability	75
Development of Membrane-Active Honokiol/Magnolol Amphiphiles as Potent Antibacterial Agents against Methicillin-Resistant Staphylococcus aureus (MRSA)	75
Perspectives on SARS-CoV-2 Main Protease Inhibitors	74
Macrocycles in Drug Discovery─Learning from the Past for the Future	73
Boosting Protein–Ligand Binding Pose Prediction and Virtual Screening Based on Residue–Atom Distance Likelihood Potential and Graph Transformer	71
Targeting SARS-CoV-2 Main Protease for Treatment of COVID-19: Covalent Inhibitors Structure–Activity Relationship Insights and Evolution Perspectives	71
Discovery of Novel Benzimidazole and Indazole Analogues as Tubulin Polymerization Inhibitors with Potent Anticancer Activities	71
The Medicinal Chemistry of Caffeine	71
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PAR	70
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities	69
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions	69
Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity	69
Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation	69
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers	69
Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer	69
Targeting Lysosomal Degradation Pathways: New Strategies and Techniques for Drug Discovery	69