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 2020-04-01 to 2024-04-01.)

Article	Citations
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight	382
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19	356
COVID-19: Drug Targets and Potential Treatments	334
U.S. FDA Approved Drugs from 2015–June 2020: A Perspective	321
Identification of the Clinical Development Candidate MRTX849, a Covalent KRAS^G12C Inhibitor for the Treatment of Cancer	297
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes	263
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19	251
Spirocyclic Scaffolds in Medicinal Chemistry	242
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS^G12D Inhibitor	242
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry	185
Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design	178
Transfer Learning for Drug Discovery	177
Inhibitors of SARS-CoV-2 Entry: Current and Future Opportunities	168
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon	166
The Most Common Functional Groups in Bioactive Molecules and How Their Popularity Has Evolved over Time	164
On the Promise of Photopharmacology Using Photoswitches: A Medicinal Chemist’s Perspective	147
Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery	146
A Decade of FDA-Approved Drugs (2010–2019): Trends and Future Directions	139
Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities	135
Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application	126
Current and Future Roles of Artificial Intelligence in Medicinal Chemistry Synthesis	117
Decision Making in Structure-Based Drug Discovery: Visual Inspection of Docking Results	114
Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis	114
Peptide–Drug Conjugates with Different Linkers for Cancer Therapy	112
Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer	111

4D-Printed Dynamic Materials in Biomedical Applications: Chemistry, Challenges, and Their Future Perspectives in the Clinical Sector	107
Learning Molecular Representations for Medicinal Chemistry	106
Rings in Clinical Trials and Drugs: Present and Future	105
Reactive Oxygen Species (ROS)-Responsive Prodrugs, Probes, and Theranostic Prodrugs: Applications in the ROS-Related Diseases	105
Design of SARS-CoV-2 PLpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity	101
Improvement in ADMET Prediction with Multitask Deep Featurization	100
Incorporating Selenium into Heterocycles and Natural Products─From Chemical Properties to Pharmacological Activities	100
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors	97
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy	95
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein	89
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy	89
Conjugated Photosensitizers for Imaging and PDT in Cancer Research	87
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP	85
Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain	83
Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras	83
Phosphine Oxides from a Medicinal Chemist’s Perspective: Physicochemical and in Vitro Parameters Relevant for Drug Discovery	81
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties	80
InteractionGraphNet: A Novel and Efficient Deep Graph Representation Learning Framework for Accurate Protein–Ligand Interaction Predictions	80
The Essential Medicinal Chemistry of Cannabidiol (CBD)	79
Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding	79
Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer	79
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer	78
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase	78
Recent Update on Development of Small-Molecule STAT3 Inhibitors for Cancer Therapy: From Phosphorylation Inhibition to Protein Degradation	77
Critical Analysis of Drug Product Recalls due to Nitrosamine Impurities	77
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models	75
Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative	75
Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development	74
3CL Protease Inhibitors with an Electrophilic Arylketone Moiety as Anti-SARS-CoV-2 Agents	73
Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy	73
Generative Models for De Novo Drug Design	72
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2	72
Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL^pro)	72
Structural Basis of AZD9291 Selectivity for EGFR T790M	71
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1)	71
Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer	71
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer	70
Recent Progress on Tubulin Inhibitors with Dual Targeting Capabilities for Cancer Therapy	70
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity	70
Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications	69
Strategies for Structural Modification of Small Molecules to Improve Blood–Brain Barrier Penetration: A Recent Perspective	69
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	69
Modulation of the Innate Immune Response by Targeting Toll-like Receptors: A Perspective on Their Agonists and Antagonists	69
Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action	69