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 2022-08-01 to 2026-08-01.)

Article	Citations
Mn-Specific Recognition of Guanidine Drives Selective Inhibition of Complex I	916
Issue Editorial Masthead	298
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy	248
Structure-Based Design and Synthesis of Covalent Inhibitors for Deubiquitinase and Acetyltransferase ChlaDUB1 of Chlamydia trachomatis	228
A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo	217
Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”	195
Navigating the Landscape of Academic Drug Discovery: An 18-Year Journey	179
Toward Dose Prediction at Point of Design	177
Targeting Toll-like Receptors 7, 8, and 9 Inhibition in Systemic Lupus Erythematosus: Therapeutic Advance and Future Directions	176
Accurate Prediction of Core-Hopping Transformations Using Molecular Dynamics-Derived Conformational Ensembles: Application to the Discovery of Novel P2X3 Antagonists	160
AKR1C3 Inhibition: A Strategy to Reverse Osimertinib Resistance in Non-small Cell Lung Cancer	138
Fragment-Based Development of Small Molecule Inhibitors Targeting Mycobacterium tuberculosis Cholesterol Metabolism	136
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2)	133
Sertraline and Astemizole Enhance the Deubiquitinase Activity of USP7 by Binding to Its Switching Loop Region	132
Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic	131
Discovery of Furan-2-Carboxylic Acid Derivatives as Novel D-Dopachrome Tautomerase (D-DT) and Macrophage Migration Inhibitory Factor-1 (MIF-1) Dual Inhibitors	130
Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1	127
Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2	125
Discovery of Covalent MLKL PROTAC Degraders via Optimization of a Theophylline Derivative Ligand for Treating Necroptosis	124
Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy	124
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1	110
From KRAS ^G12D to Pan-KRAS Inhibitors─A Journey Enabled by Synthetic Innovation and Structure-Base	106
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	106
Enhancing the Predictive Power of Machine Learning Models through a Chemical Space Complementary DEL Screening Strategy	105
Correction to “Nitroimidazole Containing [ ⁶⁸ Ga]Ga-IPM-N001 as a New CAIX-Targeting Radionuclide Tracer”	100

Multivalent Peptide-Guided EZH2 Degradation Sensitizes Immune Checkpoint Therapy in TNBC	99
Rational Design of Broad-Spectrum Non-Nucleoside Reverse Transcriptase Inhibitors via Pharmacophore-Oriented Generative Artificial Intelligence	97
Design, Synthesis, and Evaluation of Indolizine Derivatives as Nonclassical Ferroptosis Inhibitors with Efficacy in Acute Liver Injury and Ischemic Stroke Models	96
Selective and Orally Bioavailable c-Met PROTACs for the Treatment of c-Met-Addicted Cancer	95
Elaborate Structural Modifications Yielding Novel Boron-Containing N-Substituted Oseltamivir Derivatives as Potent Neuraminidase Inhibitors with Significantly Improved Broad-Spectrum Antiresistance Pr	95
Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series	94
N-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia	93
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists	92
Dissecting Structural Requirements of Leucinostatin A Derivatives for Antiprotozoal Activity and Mammalian Toxicity	92
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure−Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations	91
Optimization of Chelator Conjugation to PD-1/VEGF Bispecific Antibody for ⁸⁹ Zr-ImmunoPET Imaging	90
Small Molecule Inhibitors Targeting the “Undruggable” Survivin: The Past, Present, and Future from a Medicinal Chemist’s Perspective	90
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor	90
Rational Design of Schiff Base Copper Chelators as Potent Necroptosis Inducers for Anticancer Therapy	87
Identification of Non-competitive and Reversible Inhibitors of Glycine Transporter 2: A Promising Non-opioid Therapeutic Strategy for Neuropathic Pain	87
Cell-Based Screen Identifies a Highly Potent and Orally Available ABCB1 Modulator for Treatment of Multidrug Resistance	84
Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis	82
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation	82
Iterative Optimization and Structure–Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity	80
Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation	80
Discovery of Histone Deacetylase 8-Specific Proteolysis-Targeting Chimeras with Anticancer Activity against Hematological Malignancies	80
Macrocyclic Neutralizer to Polybrene via Direct Host–Guest Complexation	79
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	79
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor	77
Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations	77
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury	77
Efficacy, Mechanism, and Structure–Activity Relationship of 6-Methoxy Benzofuran Derivatives as a Useful Tool for Senile Osteoporosis	76
Mechanism of CRM1 Inhibition by Lansoprazole and Its Synergy with Cisplatin in Gastric Cancer	76
Structure–Activity Relationships of Truncated 1′-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs	76
Discovery of Ruthenium(II) Metallocompound and Olaparib Synergy for Cancer Combination Therapy	76
Real-Time NanoBRET Target Engagement Reveals Permeability-Activity Relationships in BET-Targeting Degraders	75
Discovery of Juglone Derivatives as Novel STAT3 Inhibitors with Potent Suppression of Cancer Cell Stemness against Breast Cancer	74
In Silico Assisted Identification, Synthesis, and In Vitro Pharmacological Characterization of Potent and Selective Blockers of the Epilepsy-Associated KCNT1 Channel	74
Issue Publication Information	74
Darizmetinib (HRX215): A Promising 1st-in-Class Liver Regenerating Drug in Phase 1b/2a Clinical Development, Targeting the Stress Signaling Protein Kinase MKK4	73
Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches	73
Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities	73
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	72
Discovery of 3-(Fluoro-imidazolyl)pyridazine Derivatives as Potent STING Agonists with Antitumor Activity	72
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach	71
Discovery of Highly Selective CYP1B1 Inhibitors	71
Multidisciplinary Training for Fostering Next-Generation Medicinal Chemists	70
Discovery of YFJ-36: Design, Synthesis, and Antibacterial Activities of Catechol-Conjugated β-Lactams against Gram-Negative Bacteria	70
Development of CD73 Inhibitors in Tumor Immunotherapy and Opportunities in Imaging and Combination Therapy	69