OOIR: Observatory of International Research

Papers

(The TQCC of ACS Medicinal Chemistry Letters is 5. 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 2021-11-01 to 2025-11-01.)

Article	Citations
Discovery of a Novel sp³-Rich M₁ Positive Allosteric Modulators (PAMs) Chemotype via Scaffold Hopping	105
Psychiatric Treatments with Short-Duration Psychedelics and AI-Driven Behavioral Monitoring	102
Azapodophyllotoxin Causes Lymphoma and Kidney Cancer Regression by Disrupting Tubulin and Monoglycerols	101
Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors	65
Novel PSMA-Targeting Radionuclide Peptidomimetics for Treating Prostate Cancer	53
Conformationally Restricted Analogues of α-Galactosylceramide as Adjuvant in COVID-19 Subunit Vaccine	52
Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2	50
From Virtual Screens to Cellular Target Engagement: New Small Molecule Ligands for the Immune Checkpoint LAG-3	47
Discovery of Tumor-Targeted 6-Methyl Substituted Pemetrexed and Related Antifolates with Selective Loss of RFC Transport	45
Clozapine as an E3 Ligand for PROTAC Technology	45
Issue Editorial Masthead	43
Issue Publication Information	39
Issue Publication Information	39
Macrocyclic Oxindole Peptide Epoxyketones─A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome	39
Cancer-Cell-Selective Targeting by Arylcyclopropylamine–Vorinostat Conjugates	38
Discovery of Selective Inhibitors of Na_V1.7 Templated on Saxitoxin as Therapeutics for Pain	37
Novel Heterocyclic Pyrimidine Derivatives as GSK3α Inhibitors	36
Introducing the Potential Binding Interface between the TRAIL-Mimicking Peptide and DR5 via Alanine Scan	36
Synthesis of Monofluorinated 7-Hydroxycoumarin-3-Carboxamides as Cell-Permeable Fluorescent Molecular Probes	35
Novel Tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders	33
In This Issue, Volume 14, Issue 5	32
Targeting the “Undruggable” Driver Protein, KRAS^G12D, as Potential Therapy in Prostate Cancer	32
Correction to “Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay”	30
Call for Papers: Fungal Pathogens – Life Cycle, Infection, Host Immunity and Drug Discovery	30
Emerging Techniques in Cancer Therapy: Precision Targeting for Improved Outcomes	29

Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology	29
Novel Phosphorylpurinone Compounds for Treating Cancer	29
Application of Deuterated N,N-Dimethyltryptamine in the Potential Treatment of Psychiatric and Neurological Disorders	28
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach	28
Polybromo-1 Bromodomain Inhibitor Selectivity Is Mediated by a Unique Ligand-Binding Pocket	27
Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1–Nrf2 PPI Inhibitor	27
Bispecific Antibodies Produced via Chemical Site-Specific Conjugation Technology: AJICAP Second-Generation	27
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation	27
Design and Synthesis of a Structurally Stabilized B-Chain Antagonist Targeting Relaxin Family Peptide Receptor 3 (RXFP3)	27
Tryptamines and Mental Health: Activating the 5-HT Receptor for Therapeutic Potential	26
Contemporary Computational Applications and Tools in Drug Discovery	26
Virtual Screening-Guided Discovery of Small-Molecule CHI3L1 Inhibitors with Functional Activity in Glioblastoma Spheroids	25
Targeting Cancer: A New Era in Cancer Therapy through Immune Fitness Modulation and KRAS Degradation	25
Novel Triazines as NLRP3 Inhibitors for Treating Multiple Diseases	24
SAR Study of 4,8-Disubstituted Pyrimido[5,4-d]pyrimidines Exhibiting Antitrypanosomal and Antileishmanial Activity	24
Discovery of Pyrazole-Containing 4-Arylindolines as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction	23
Tricyclic and Novel Chemotypes as Selective WRN Helicase Inhibitors for MSI-H Cancer Therapy	23
Novel Papain-Like Protease Inhibitors for Treating Viral Infections, in Particular Coronavirus Infections	22
Announcing the Early Career Board of ACS Medicinal Chemistry Letters	22
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents	22
Issue Editorial Masthead	21
In Retrospect: Root-Cause Analysis of Structure–Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833)	21
Fused Bicyclic Heteroaryl Compounds as NLRP3 Inhibitors for Treating Asthma or COPD	21
An Automated Purification Workflow Coupled with Material-Sparing High-Throughput ¹H NMR for Parallel Medicinal Chemistry	20
Synthesis and In Vitro/In Silico α-Glucosidase Inhibitory Study of Novel Ethanones Containing Naphthalene-Linked 1,2,4-Triazole	20
Neuropharmacological Advances: Harnessing 5-HT2A Receptor Modulators and Psychoplastogens	20
Thermal Stability and Utility of Dienes as Protecting Groups for Acrylamides	20
Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers	20
Quantum Mechanics-Based Ranking of Predicted Proteolysis Targeting Chimeras-Mediated Ternary Complexes	19
Enantioselective Bioreduction of Medicinally Relevant Nitrogen-Heteroaromatic Ketones	19
Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2	19
Heparan Sulfate-Mimicking Glycopolymers Bind SARS-CoV-2 Spike Protein in a Length- and Sulfation Pattern-Dependent Manner	19
ACS Medicinal Chemistry Letters Patent Highlights: A Look Back	18
N-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents	18
Evaluating the Diversity and Target Addressability of DELs using Scaffold Analysis and Machine Learning	18
Discovery of N-(4-(Aminomethyl)phenyl)-5-methylpyrimidin-2-amine Derivatives as Potent and Selective JAK2 Inhibitors	18
An Estrogen Receptor β Agonist with AR Antagonist Activity from a Modern Asymmetric De Novo Steroid Synthesis	18
Novel 3-Cycloaminoindole Compounds as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders	18
Targeting Oncogenic Pathways: Advances in KRAS, CDK, EGFR, and PROTAC-Based Therapies	18
3AcFNP-59 for Positron Emission Tomography Imaging of Cholesterol Trafficking and Utilization	18
Synthesis and Evaluation of Halogenated Pralidoximes in Reactivation of Organophosphate-Inhibited Cholinesterases	17
In-Silico Screening-Based Discovery of New Natural eEF2K Inhibitors with Neuritogenic Activity	17
Thermal Degradation Kinetics and pH–Rate Profile of Verbascoside and Stability Improvement by Solid Lipid Nanoparticles	17
Optimized Parenteral and Intranasal Formulations of Tryptamine Psychedelics for Rapid-Acting Antidepressant Therapy	17
Constructive On-DNA Abramov Reaction and Pudovik Reaction for DEL Synthesis	17
Discovery of Novel MTA-Cooperative PRMT5 Inhibitors with a 2,3-Dihydro-1H-imidazo[1,2-b]pyrazole Scaffold	17
The Synergistic Effects of 5-HT2A and TRP Agonism/Antagonism in Reducing Inflammation for Enhanced Mental and Physical Health	16
Identification of an Allene Warhead That Selectively Targets a Histidine Residue in the Escherichia coli Oxidoreductase Enzyme DsbA	16
Fragment Ligands of the m⁶A-RNA Reader YTHDF2	16
Fragment-Based Dynamic Combinatorial Chemistry for Identification of Selective α-Glucosidase Inhibitors	16

Synthesis and Preclinical Evaluation of Novel ⁶⁸Ga-DOTA-RBB as Potential PET Radiotracer for Imaging CDK4/6 in Tumors	16
Novel Piperidinylpyridinylcarbonitrile Derivatives as QPCT and QPCTL Inhibitors for Treating Cancer	16
Piperazinobenzodiazepinones: New Encephalitic Alphavirus Inhibitors via Ring Expansion of 2-Dichloromethylquinazolinones	16
Homogeneous Dual-Payload Antibody-Drug Conjugates Produced by Combined Distinct Conjugation Strategies	16
Exploiting Solvent Exposed Salt-Bridge Interactions for the Discovery of Potent Inhibitors of SOS1 Using Free-Energy Perturbation Simulations	15
Discovery of a Potent and Highly Selective Inhibitor of Aurora A Kinase	15
Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20	15
Machine Learning ADME Models in Practice: Four Guidelines from a Successful Lead Optimization Case Study	15
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists	15
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson’s Disease	15
Novel Compounds as 5-HT2A Receptor Modulators for Treating Psychiatric and Neurological Disorders	15
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2	15
(−)-Epigallocatechin Gallate is a Noncompetitive Inhibitor of NAD Kinase	15
Novel Isoindolinone-Containing PARP Inhibitors: Synthesis and Therapeutic Applications in CNS Cancer Treatment	15
Identification and Exploration of a Series of SARS-Cov-2 M^Pro Cyano-Based Inhibitors Revealing Ortho-Substitution Effects within the P3 Biphenyl Group	15
Advancing New Chemical Modalities into Clinical Studies	15
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2	15
Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones Active against Plasmodium and Trypanosomatids	14
Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids	14
Issue Publication Information	14
Issue Publication Information	14
Novel Indole Derivatives as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders	14
Design, Synthesis, and Biological Activity of l-1′-Homologated Adenosine Derivatives	14
Structure-Guided Temporin L Analogs Development to Inhibit the Main Protease of SARS-CoV-2	14
Small Molecules Blocking the Assembly of TCAB1 and Telomerase Complexes: Lead Discovery and Biological Activity	14
Lipase-Catalyzed Synthesis and Biological Evaluation of N-Picolineamides as Trypanosoma cruzi Antiproliferative Agents	14
Issue Editorial Masthead	14
Issue Editorial Masthead	14
Proline Homologation in Melanostatin Neuropeptide: Discovery of Potent Modulators of the Dopamine D₂ Receptors	14
Issue Editorial Masthead	14
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties	14
Discovery of Pyridone-Substituted Triazolopyrimidine Dual A_2A/A₁ AR Antagonists for the Treatment of Ischemic Stroke	14
Issue Publication Information	14
Exploring the Therapeutic Potential of Entheogens in Postoperative Cognitive Decline and Psychological Resilience	14
2-Aminoimidazole-benzimidazole Conjugates Potentiate the Gram-Positive Selective Antibiotic Clarithromycin against Acinetobacter baumannii	14
Pharmacophore-Based Structure Optimization of S-Trityl-l-Cysteine Derivatives for Cytotoxic Payload Applications	14
Discovery of Potent and Oral Bioavailable MAT2A Inhibitors for the Treatment of MTAP-Deleted Tumors	13
In Silico Optimized Stapled Peptides Targeting WASF3 in Breast Cancer	13
Discovery of First-in-Class BAZ2A/B and BAZ2B-Selective Degraders	13
Identification and Preliminary Characterization of a Novel Tasquinimod Analog that Unexpectedly Induces Mitotic Arrest by Alteration of Microtubule Dynamics	13
Targeted Degradation of Androgen Receptor for the Potential Treatment of Prostate Cancer	13
The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib–GV1001 Conjugate	13
Novel Imidazotriazine Derivatives as IL-17 Modulators for Treating Inflammatory and Autoimmune Disorders	13
In the Quest for Potent and Selective Malic Enzyme 3 Inhibitors for the Treatment of Pancreatic Ductal Adenocarcinoma	13
SiRNAs with Neutral Phosphate Triester Hydrocarbon Tails Exhibit Carrier-Free Gene-Silencing Activity	13
Photoaffinity Probe Reveals the Potential Target of Harringtonolide for Cancer Cell Migration Inhibition	13
Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT_2A Receptor Agonist	13
Identification and In Silico Binding Study of a Highly Potent DENV NS2B-NS3 Covalent Inhibitor	13
Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy	13
Novel Furopyridine and Furopyrimidine Compounds as PI4K Inhibitors for Treating Malaria and Viral Infection	13
Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR₇ Allosteric Agonist	12
Innovative Psychedelic Therapies: Harnessing 5-MeO-DMT and DMT for Mental Health Treatment	12
Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055	12
Re-evaluation of Cyclic Peptide Binding to Neurotensin Receptor 1 by Shifting the Peptide Register during Synthesis	12
Identification of Boc₂Lys-Linked Ethacrynic Acid and Its Analogues As Efficient Glutathione S-Transferase Degraders	12
Novel Nonpeptide as Oxytocin Receptor Agonist	12
Pyrroloquinolone-Based Compounds as a Novel Antimycobacterial Chemotype	12
Novel Fused Heterocycles as 5-HT2A Receptor Agonists for Treating Neurological Diseases, Namely, Depression, Anxiety, Substance Abuse, and Headaches	12
Hybrids of Membrane-Translocating Antimicrobial Peptides Show Enhanced Activity through Membrane Permeabilization	12
Novel Pyrimidinyl Sulfonamide Derivatives as GPR17 Modulators	12
Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors	12
In this Issue, Volume 16, Issue 5	12
Fragment-Based Discovery of Drug-like LRH-1 Agonists	12
Glycine Betaine-Functionalized Ionic Liquids: Design of Versatile Bioplatform for Incorporating Biologically Active Moieties into Cations	12
Structure–Activity Relationships for the N-Me- Versus N-H-Amide Modification to Macrocyclic ent-Verticilide Antiarrhythmics	12
Synthesis and Evaluation of Novel meso-Tetraphenyltetrabenzoporphyrins for Photodynamic Therapy	12
Design, Synthesis, and Evaluation of 8-(o-Tolyl)quinazoline Derivatives as Small-Molecule PD-1/PD-L1 Antagonists	12
Novel Substituted Pyrazoles as 5-HT1A Agonists for Treating Neuropsychiatric Diseases	12
Structure-Guided Virtual Screening of Small Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy	11
Tetrazole Derivatives as TRPA1 Inhibitors for Treating Idiopathic Lung Disease or Cough	11
Issue Publication Information	11
Discovery of Small-Molecule Ligands for the E3 Ligase STUB1/CHIP from a DNA-Encoded Library Screen	11
Targeted Degradation of Histone Deacetylases via Bypassing E3 Ligase Targeting Chimeras (BYETACs)	11
In This Issue, Volume 13, Issue 1	11
Recent Developments in Mass Spectrometry to Support Next-Generation Synthesis and Screening	11
Novel Pyridazin-3(2H)-one-Based Guanidine Derivatives as Potential DNA Minor Groove Binders with Anticancer Activity	11
Property-Based Optimization of Cereblon-Based Molecular Glue Degraders	11
Issue Publication Information	11
Application of Rapidly Accelerating Fibrosarcoma Protein Degraders in Drug Discovery	11
Synthesis and Monoamine Oxidase Inhibitory Activity of Halogenated Flavones	11

Peripherally Restricted Fused Heterocyclic Peptidomimetic Multifunctional Opioid Agonists as Novel, Potent Analgesics	11
Novel Compounds as 5-HT2A Agonists for Treating Mental Illness or CNS Disorders	11
Novel N-Substituted Indole Derivatives as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders	11
Potentiometric Determination of Acid Dissociation Constants (pK_a) for an Anticancer Pyrrole-Imidazole Polyamide	10
Synthesis and Evaluation of Benzylamine Inhibitors of Neuropathogenic Naegleria fowleri “Brain-Eating” Amoeba	10
Enantiopure Benzofuran-2-carboxamides of 1-Aryltetrahydro-β-carbolines Are Potent Antimalarials In Vitro	10
Inhibitors of the Cyclic GMP-AMP Synthase (cGAS) as Potential Treatment for Autoimmune and Inflammatory Diseases	10
Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery	10
Reducing Self-Assembly by Increasing Net Charge: Effect on Biological Activity of Mastoparan C	10
4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL	10
Correction to “Study of Chalcogen Aspirin Derivatives with Carbonic Anhydrase Inhibitory Properties for Treating Inflammatory Pain”	10
Structure–Activity Relationship Study of 1H-Pyrrole-3-carbonitrile Derivatives as STING Receptor Agonists	10
Next-Generation GLUT Inhibitors: Lactone to Lactam Conversion in Rapaglutin A Confers Resistance to Plasma Esterases	10
Decarboxylative Cross-Coupling: A Radical Tool in Medicinal Chemistry	10
Broad-Spectrum Antimicrobial Efficacy of Cyclic Antimicrobial Peptide Against Multidrug-Resistant Staphylococcus aureus Infections	10
Bioisostere Effects on the EPSA of Common Permeability-Limiting Groups	10
Novel Pyridine Derivatives as 5-HT2A Agonists for Treating Psychiatric Disorders	10
9,10-Bis[(4-(2-hydroxyethyl)piperazine-1-yl)prop2-yne-1-yl]anthracene: G-Quadruplex Selectivity and Anticancer Activity	10
N-Biphenyl Pyrrolinones and Dibenzofurans as RNA-Binding Protein LIN28 Inhibitors Disrupting the LIN28–Let-7 Interaction	10
Issue Publication Information	10
Amino-cyclohexane Carboxylic Acid Inhibitors of Arginase	10
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field	10
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR^T790M/C797S Mutants	10
Accelerated Discovery of Macrocyclic CDK2 Inhibitor QR-6401 by Generative Models and Structure-Based Drug Design	10
Issue Editorial Masthead	10
Issue Editorial Masthead	10
Recent Discovery of PARP7 Inhibitors as Anticancer Agents	10
Issue Publication Information	10
A Neutral Flavin–Triphenylamine Probe for Mitochondrial Bioimaging under Different Microenvironments	9
Structure-Based Design of Novel TLR7/8 Agonist Payloads Enabling an Immunomodulatory Conjugate Approach	9
NMR-Based Fragment Screen of the von Hippel-Lindau Elongin C&B Complex	9
Discovery of Indole-Based PDE5 Inhibitors: Synthesis and Pharmacological Evaluation	9
Novel Aminocyclobutanes as Monoacylglycerol Lipase Modulators	9
Novel Lactams as Cbl-b Inhibitors for Treating Cancer	9
Biological Effects of Modifications of the Englerin A Glycolate	9
Novel Piperidine Substituted Pyrazolopyrimidine Derivatives as SGK1 Inhibitors for Treating Cardiovascular Diseases	9
Relevance of the Trillion-Sized Chemical Space “eXplore” as a Source for Drug Discovery	9
Discovery of Non-Covalent Inhibitors for SARS-CoV-2 PLpro: Integrating Virtual Screening, Synthesis, and Experimental Validation	9
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2–p53 Inhibitor	9
Discovery of Kinesin KIF18A Inhibitor ATX020: Tactical Application of Silicon Atom Replacement	9
Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries	9
Synthesis and Determination of Anticancer Activity of Dicobalt Hexacarbonyl 2′-Deoxy-5-alkynylfuropyrimidines	9
Selective Wee1 Inhibitors Led to Antitumor Activity In Vitro and Correlated with Myelosuppression	9
How a Blockchain Approach Can Improve Data Reliability in the COVID-19 Pandemic	9
In This Issue, Volume 12, Issue 11	9
MALT1 Inhibitors for Treating Cancer and Immunological Diseases	9
Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release	9
Novel Compounds as NLRP3 Inhibitors for Treating Asthma or COPD	9
The Inhibitors of Mucosa-Associated Lymphoid Tissue Lymphoma Translocation Protein 1 (MALT-1) Protease as Potential Treatment of ABC-DLBCL and Similar Diseases	9
Discovery of Novel Pyrimidine Derivatives as Human Pin1 Covalent Inhibitors	9
A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir	9
Discovery of INCB126503 as a Potent and Selective FGFR2/3 Inhibitor	9
Discovery of Novel Hydroxyimine-Tethered Benzenesulfonamides as Potential Human Carbonic Anhydrase IX/XII Inhibitors	9
Steroid–Quinoline Hybrids for Disruption and Reversion of Protein Aggregation Processes	9
Inhibitors of Na_v1.7 for the Treatment of Pain	9
Discovery of Selective Aldehyde Dehydrogenase Inhibitors for the Treatment of Cancer	9
Development of BODIPY FL SNS 032 as a Versatile Probe for Constitutive Androstane Receptor and Multiple Kinases	9
Novel 2-Pyrrolidone Derivatives as Negative Allosteric Modulators of GluN2B-Containing NMDA Receptors	9
ACS Medicinal Chemistry Letters: An Innovation Ten Years in the Making	9
Mining Druggable Sites in Influenza A Hemagglutinin: Binding of the Pinanamine-Based Inhibitor M090	9
Pioneering Changes in Psychiatry: Biomarkers, Psychedelics, and AI	9
Potent, Selective, and Orally Bioavailable Quinazoline-Based STK17A/B Dual Inhibitors	9
Radiosynthesis and Preclinical Evaluation of a Carbon-11 Labeled Phosphodiesterase 7 Inhibitor for PET Neuroimaging	8
Novel Thienopyrrole Compounds for Treating Autoimmune Diseases and Inflammatory Conditions	8
Issue Publication Information	8
Issue Publication Information	8
A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors	8
Total Synthesis as Training for Medicinal Chemistry	8
In This Issue, Volume 15, Issue 4	8
Ligand Design with Accelerated Disulfide Formation with Serum Albumin to Extend Blood Retention	8
BTZ-Derived Benzisothiazolinones with In Vitro Activity against Mycobacterium tuberculosis	8
Structure–Activity Relationship of Anti-Mycobacterium abscessus Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors	8
Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists	8
Innovations in Precision Oncology: Biomarker-Driven Approaches for Enhanced Cancer Therapy	8
Novel AHR Agonists for Treating Psoriasis	8
Issue Publication Information	8
Addition to “The Death of the Strategy of Classical Chiral Switches Is an Exaggeration”	8
Identification of 5-Thiocyanatothiazol-2-amines Disrupting WDR5-MYC Protein–Protein Interactions	8
Optimization of Brain Penetrant SARM1 Orthosteric Inhibitors and Discovery of Their Paradoxical Subinhibitory Activation	8
Design and Assessment of First-Generation Heterobifunctional PPARα/STING Modulators	8
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode	8
Application of Compositions Comprising a KRAS G12C Inhibitor and an EGFR Inhibitor for the Potential Treatment of Cancer	8
Cytosolic Enzymes Generate Cannabinoid Metabolites 7-Carboxycannabidiol and 11-Nor-9-carboxytetrahydrocannabinol	8
Readily Accessible High-Throughput Experimentation: A General Protocol for the Preparation of ChemBeads and EnzyBeads	8
Call for Papers: Exploring the Use of AI/ML Technologies in Medicinal Chemistry and Drug Discovery	8
Integrated Advancements in Neuroplasticity, Psychedelic Therapeutics, and AI-Driven Innovations for Precision Medicine	8
Development of Conformationally Restricted Negamycin Derivatives for Potent Readthrough Activity	8
Issue Editorial Masthead	8
Bicyclic Inhibitors of Branched-Chain α-Keto Acid Dehydrogenase Kinase (BDK) with In Vivo Activity	8
Structural Evaluations of a Selective Human STING^A230 Agonist and Its Use in Macrophage Immunotherapies	8
Novel Ergoline Compounds as 5-HT2A Agonists for Treating Mood Disorders Such as Depressive Disorders and Bipolar Disorders	8
Exploring the 1-(4-Nitrophenyl)-3-arylprop-2-en-1-one Scaffold for the Selective Inhibition of Monoamine Oxidase B	8
Integrating Neuroprotective and Anti-inflammatory Strategies in the Development of PI3K Inhibitors for Enhanced Cancer Therapy	8
Novel 6-Substituted-3-Phenylisoindolin-1-ones as Cbl-B Inhibitors for Treating Cancer	8
Novel Bicyclic Heterocycles as MRGPRX2 Antagonists for Treating Inflammatory Diseases	8