ACS Medicinal Chemistry Letters

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 2021-12-01 to 2025-12-01.)
ArticleCitations
Psychiatric Treatments with Short-Duration Psychedelics and AI-Driven Behavioral Monitoring111
Azapodophyllotoxin Causes Lymphoma and Kidney Cancer Regression by Disrupting Tubulin and Monoglycerols107
Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors104
Conformationally Restricted Analogues of α-Galactosylceramide as Adjuvant in COVID-19 Subunit Vaccine69
Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD256
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach55
Discovery of Tumor-Targeted 6-Methyl Substituted Pemetrexed and Related Antifolates with Selective Loss of RFC Transport50
Issue Publication Information47
Issue Editorial Masthead47
Issue Publication Information45
Macrocyclic Oxindole Peptide Epoxyketones─A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome43
Discovery of Selective Inhibitors of NaV1.7 Templated on Saxitoxin as Therapeutics for Pain41
Cancer-Cell-Selective Targeting by Arylcyclopropylamine–Vorinostat Conjugates41
Introducing the Potential Binding Interface between the TRAIL-Mimicking Peptide and DR5 via Alanine Scan39
Synthesis of Monofluorinated 7-Hydroxycoumarin-3-Carboxamides as Cell-Permeable Fluorescent Molecular Probes39
Novel Heterocyclic Pyrimidine Derivatives as GSK3α Inhibitors38
Novel Tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders37
In This Issue, Volume 14, Issue 536
Targeting the “Undruggable” Driver Protein, KRASG12D, as Potential Therapy in Prostate Cancer36
Call for Papers: Fungal Pathogens – Life Cycle, Infection, Host Immunity and Drug Discovery35
Correction to “Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay”33
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology32
Novel Phosphorylpurinone Compounds for Treating Cancer32
Application of Deuterated N,N-Dimethyltryptamine in the Potential Treatment of Psychiatric and Neurological Disorders31
Bispecific Antibodies Produced via Chemical Site-Specific Conjugation Technology: AJICAP Second-Generation31
Clozapine as an E3 Ligand for PROTAC Technology30
Polybromo-1 Bromodomain Inhibitor Selectivity Is Mediated by a Unique Ligand-Binding Pocket30
Design and Synthesis of a Structurally Stabilized B-Chain Antagonist Targeting Relaxin Family Peptide Receptor 3 (RXFP3)30
Emerging Techniques in Cancer Therapy: Precision Targeting for Improved Outcomes29
Discovery of a Novel sp3-Rich M1 Positive Allosteric Modulators (PAMs) Chemotype via Scaffold Hopping29
Virtual Screening-Guided Discovery of Small-Molecule CHI3L1 Inhibitors with Functional Activity in Glioblastoma Spheroids29
Novel PSMA-Targeting Radionuclide Peptidomimetics for Treating Prostate Cancer28
From Virtual Screens to Cellular Target Engagement: New Small Molecule Ligands for the Immune Checkpoint LAG-328
Tryptamines and Mental Health: Activating the 5-HT Receptor for Therapeutic Potential27
Contemporary Computational Applications and Tools in Drug Discovery27
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation27
Novel Triazines as NLRP3 Inhibitors for Treating Multiple Diseases26
Targeting Cancer: A New Era in Cancer Therapy through Immune Fitness Modulation and KRAS Degradation26
Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1–Nrf2 PPI Inhibitor26
Tricyclic and Novel Chemotypes as Selective WRN Helicase Inhibitors for MSI-H Cancer Therapy25
SAR Study of 4,8-Disubstituted Pyrimido[5,4-d]pyrimidines Exhibiting Antitrypanosomal and Antileishmanial Activity25
Discovery of Pyrazole-Containing 4-Arylindolines as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction24
Announcing the Early Career Board of ACS Medicinal Chemistry Letters24
Issue Editorial Masthead23
In Retrospect: Root-Cause Analysis of Structure–Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833)23
Novel Papain-Like Protease Inhibitors for Treating Viral Infections, in Particular Coronavirus Infections23
Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers22
Fused Bicyclic Heteroaryl Compounds as NLRP3 Inhibitors for Treating Asthma or COPD22
Thermal Stability and Utility of Dienes as Protecting Groups for Acrylamides21
An Automated Purification Workflow Coupled with Material-Sparing High-Throughput 1H NMR for Parallel Medicinal Chemistry21
Synthesis and In Vitro/In Silico α-Glucosidase Inhibitory Study of Novel Ethanones Containing Naphthalene-Linked 1,2,4-Triazole21
Neuropharmacological Advances: Harnessing 5-HT2A Receptor Modulators and Psychoplastogens21
Novel 3-Cycloaminoindole Compounds as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders20
Enantioselective Bioreduction of Medicinally Relevant Nitrogen-Heteroaromatic Ketones20
Discovery of N-(4-(Aminomethyl)phenyl)-5-methylpyrimidin-2-amine Derivatives as Potent and Selective JAK2 Inhibitors20
Quantum Mechanics-Based Ranking of Predicted Proteolysis Targeting Chimeras-Mediated Ternary Complexes20
ACS Medicinal Chemistry Letters Patent Highlights: A Look Back20
Heparan Sulfate-Mimicking Glycopolymers Bind SARS-CoV-2 Spike Protein in a Length- and Sulfation Pattern-Dependent Manner20
3AcFNP-59 for Positron Emission Tomography Imaging of Cholesterol Trafficking and Utilization19
Machine Learning ADME Models in Practice: Four Guidelines from a Successful Lead Optimization Case Study19
N-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents19
Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC2019
An Estrogen Receptor β Agonist with AR Antagonist Activity from a Modern Asymmetric De Novo Steroid Synthesis18
Optimized Parenteral and Intranasal Formulations of Tryptamine Psychedelics for Rapid-Acting Antidepressant Therapy18
Thermal Degradation Kinetics and pH–Rate Profile of Verbascoside and Stability Improvement by Solid Lipid Nanoparticles18
Discovery of Novel MTA-Cooperative PRMT5 Inhibitors with a 2,3-Dihydro-1H-imidazo[1,2-b]pyrazole Scaffold18
Piperazinobenzodiazepinones: New Encephalitic Alphavirus Inhibitors via Ring Expansion of 2-Dichloromethylquinazolinones18
The Synergistic Effects of 5-HT2A and TRP Agonism/Antagonism in Reducing Inflammation for Enhanced Mental and Physical Health18
In-Silico Screening-Based Discovery of New Natural eEF2K Inhibitors with Neuritogenic Activity18
Identification of an Allene Warhead That Selectively Targets a Histidine Residue in the Escherichia coli Oxidoreductase Enzyme DsbA17
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson’s Disease17
Novel Isoindolinone-Containing PARP Inhibitors: Synthesis and Therapeutic Applications in CNS Cancer Treatment17
Identification and Exploration of a Series of SARS-Cov-2 MPro Cyano-Based Inhibitors Revealing Ortho-Substitution Effects within the P3 Biphenyl Group17
Novel Piperidinylpyridinylcarbonitrile Derivatives as QPCT and QPCTL Inhibitors for Treating Cancer17
Homogeneous Dual-Payload Antibody-Drug Conjugates Produced by Combined Distinct Conjugation Strategies17
Exploiting Solvent Exposed Salt-Bridge Interactions for the Discovery of Potent Inhibitors of SOS1 Using Free-Energy Perturbation Simulations17
Discovery of a Potent and Highly Selective Inhibitor of Aurora A Kinase17
Advancing New Chemical Modalities into Clinical Studies17
Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 216
Fragment Ligands of the m6A-RNA Reader YTHDF216
Novel Compounds as 5-HT2A Receptor Modulators for Treating Psychiatric and Neurological Disorders16
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 216
Constructive On-DNA Abramov Reaction and Pudovik Reaction for DEL Synthesis16
Evaluating the Diversity and Target Addressability of DELs using Scaffold Analysis and Machine Learning16
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists16
Fragment-Based Dynamic Combinatorial Chemistry for Identification of Selective α-Glucosidase Inhibitors15
(−)-Epigallocatechin Gallate is a Noncompetitive Inhibitor of NAD Kinase15
Issue Editorial Masthead15
Issue Editorial Masthead15
Proline Homologation in Melanostatin Neuropeptide: Discovery of Potent Modulators of the Dopamine D2 Receptors15
Synthesis and Evaluation of Halogenated Pralidoximes in Reactivation of Organophosphate-Inhibited Cholinesterases15
Targeting Oncogenic Pathways: Advances in KRAS, CDK, EGFR, and PROTAC-Based Therapies15
Issue Publication Information15
Exploring the Therapeutic Potential of Entheogens in Postoperative Cognitive Decline and Psychological Resilience15
2-Aminoimidazole-benzimidazole Conjugates Potentiate the Gram-Positive Selective Antibiotic Clarithromycin against Acinetobacter baumannii15
Synthesis and Preclinical Evaluation of Novel 68Ga-DOTA-RBB as Potential PET Radiotracer for Imaging CDK4/6 in Tumors15
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK215
Issue Publication Information15
Novel Indole Derivatives as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders15
Issue Publication Information15
Structure-Guided Temporin L Analogs Development to Inhibit the Main Protease of SARS-CoV-214
Discovery of Pyridone-Substituted Triazolopyrimidine Dual A2A/A1 AR Antagonists for the Treatment of Ischemic Stroke14
Identification and Preliminary Characterization of a Novel Tasquinimod Analog that Unexpectedly Induces Mitotic Arrest by Alteration of Microtubule Dynamics14
Targeted Degradation of Androgen Receptor for the Potential Treatment of Prostate Cancer14
Issue Editorial Masthead14
Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones Active against Plasmodium and Trypanosomatids14
Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids14
The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib–GV1001 Conjugate14
Novel Imidazotriazine Derivatives as IL-17 Modulators for Treating Inflammatory and Autoimmune Disorders14
Pharmacophore-Based Structure Optimization of S-Trityl-l-Cysteine Derivatives for Cytotoxic Payload Applications14
Small Molecules Blocking the Assembly of TCAB1 and Telomerase Complexes: Lead Discovery and Biological Activity14
In Silico Optimized Stapled Peptides Targeting WASF3 in Breast Cancer14
Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT2A Receptor Agonist14
Lipase-Catalyzed Synthesis and Biological Evaluation of N-Picolineamides as Trypanosoma cruzi Antiproliferative Agents14
Discovery of Potent and Oral Bioavailable MAT2A Inhibitors for the Treatment of MTAP-Deleted Tumors13
In the Quest for Potent and Selective Malic Enzyme 3 Inhibitors for the Treatment of Pancreatic Ductal Adenocarcinoma13
Identification and In Silico Binding Study of a Highly Potent DENV NS2B-NS3 Covalent Inhibitor13
Structure–Activity Relationships for the N-Me- Versus N-H-Amide Modification to Macrocyclic ent-Verticilide Antiarrhythmics13
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties13
Novel Pyrimidinyl Sulfonamide Derivatives as GPR17 Modulators13
In this Issue, Volume 16, Issue 513
Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy13
Photoaffinity Probe Reveals the Potential Target of Harringtonolide for Cancer Cell Migration Inhibition13
Hybrids of Membrane-Translocating Antimicrobial Peptides Show Enhanced Activity through Membrane Permeabilization13
Discovery of First-in-Class BAZ2A/B and BAZ2B-Selective Degraders13
Synthesis and Evaluation of Novel meso-Tetraphenyltetrabenzoporphyrins for Photodynamic Therapy13
Novel Substituted Pyrazoles as 5-HT1A Agonists for Treating Neuropsychiatric Diseases13
Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-1105513
Novel Furopyridine and Furopyrimidine Compounds as PI4K Inhibitors for Treating Malaria and Viral Infection13
Design, Synthesis, and Biological Activity of l-1′-Homologated Adenosine Derivatives13
SiRNAs with Neutral Phosphate Triester Hydrocarbon Tails Exhibit Carrier-Free Gene-Silencing Activity13
Re-evaluation of Cyclic Peptide Binding to Neurotensin Receptor 1 by Shifting the Peptide Register during Synthesis13
Innovative Psychedelic Therapies: Harnessing 5-MeO-DMT and DMT for Mental Health Treatment13
Fragment-Based Discovery of Drug-like LRH-1 Agonists12
Application of Rapidly Accelerating Fibrosarcoma Protein Degraders in Drug Discovery12
Synthesis and Monoamine Oxidase Inhibitory Activity of Halogenated Flavones12
Issue Publication Information12
Novel Fused Heterocycles as 5-HT2A Receptor Agonists for Treating Neurological Diseases, Namely, Depression, Anxiety, Substance Abuse, and Headaches12
Tetrazole Derivatives as TRPA1 Inhibitors for Treating Idiopathic Lung Disease or Cough12
Novel Pyridazin-3(2H)-one-Based Guanidine Derivatives as Potential DNA Minor Groove Binders with Anticancer Activity12
Recent Developments in Mass Spectrometry to Support Next-Generation Synthesis and Screening12
Pyrroloquinolone-Based Compounds as a Novel Antimycobacterial Chemotype12
Glycine Betaine-Functionalized Ionic Liquids: Design of Versatile Bioplatform for Incorporating Biologically Active Moieties into Cations12
In This Issue, Volume 13, Issue 112
Structure-Guided Virtual Screening of Small Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy12
Discovery of CVN636 : A Highly Potent, Selective, and CNS Penetrant mGluR 7 Allosteric Agonist11
Targeted Degradation of Histone Deacetylases via Bypassing E3 Ligase Targeting Chimeras (BYETACs)11
Discovery of Small-Molecule Ligands for the E3 Ligase STUB1/CHIP from a DNA-Encoded Library Screen11
Property-Based Optimization of Cereblon-Based Molecular Glue Degraders11
Reducing Self-Assembly by Increasing Net Charge: Effect on Biological Activity of Mastoparan C11
Inhibitors of the Cyclic GMP-AMP Synthase (cGAS) as Potential Treatment for Autoimmune and Inflammatory Diseases11
Novel N-Substituted Indole Derivatives as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders11
Novel Compounds as 5-HT2A Agonists for Treating Mental Illness or CNS Disorders11
Amino-cyclohexane Carboxylic Acid Inhibitors of Arginase11
Design, Synthesis, and Evaluation of 8-(o-Tolyl)quinazoline Derivatives as Small-Molecule PD-1/PD-L1 Antagonists11
Peripherally Restricted Fused Heterocyclic Peptidomimetic Multifunctional Opioid Agonists as Novel, Potent Analgesics11
Issue Editorial Masthead11
Targeted Degradation of EGFR and PKC Isoforms: Emerging Bifunctional and Peptidic Modalities in Oncology and Immune Regulation11
Novel 2 H -Pyrazolo[3,4- d ]thiazole Compounds Targeting NLRP3 for the Treatment of Neurodegenerative Dise10
Decarboxylative Cross-Coupling: A Radical Tool in Medicinal Chemistry10
Potentiometric Determination of Acid Dissociation Constants (pKa) for an Anticancer Pyrrole-Imidazole Polyamide10
Synthesis and Evaluation of Benzylamine Inhibitors of Neuropathogenic Naegleria fowleri “Brain-Eating” Amoeba10
Novel Compounds as NLRP3 Inhibitors for Treating Asthma or COPD10
N-Biphenyl Pyrrolinones and Dibenzofurans as RNA-Binding Protein LIN28 Inhibitors Disrupting the LIN28–Let-7 Interaction10
Pioneering Changes in Psychiatry: Biomarkers, Psychedelics, and AI10
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFRT790M/C797S Mutants10
Recent Discovery of PARP7 Inhibitors as Anticancer Agents10
Broad-Spectrum Antimicrobial Efficacy of Cyclic Antimicrobial Peptide Against Multidrug-Resistant Staphylococcus aureus Infections10
Issue Publication Information10
Bioisostere Effects on the EPSA of Common Permeability-Limiting Groups10
Identification of Boc2Lys-Linked Ethacrynic Acid and Its Analogues As Efficient Glutathione S-Transferase Degraders10
Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery10
Accelerated Discovery of Macrocyclic CDK2 Inhibitor QR-6401 by Generative Models and Structure-Based Drug Design10
Development of BODIPY FL SNS 032 as a Versatile Probe for Constitutive Androstane Receptor and Multiple Kinases10
Issue Editorial Masthead10
Synthesis and Determination of Anticancer Activity of Dicobalt Hexacarbonyl 2′-Deoxy-5-alkynylfuropyrimidines10
Enantiopure Benzofuran-2-carboxamides of 1-Aryltetrahydro-β-carbolines Are Potent Antimalarials In Vitro10
Correction to “Study of Chalcogen Aspirin Derivatives with Carbonic Anhydrase Inhibitory Properties for Treating Inflammatory Pain”10
Issue Editorial Masthead10
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field10
4-Oxo-β-lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL10
Novel Nonpeptide as Oxytocin Receptor Agonist10
Novel Piperidine Substituted Pyrazolopyrimidine Derivatives as SGK1 Inhibitors for Treating Cardiovascular Diseases10
Next-Generation GLUT Inhibitors: Lactone to Lactam Conversion in Rapaglutin A Confers Resistance to Plasma Esterases10
Novel Pyridine Derivatives as 5-HT2A Agonists for Treating Psychiatric Disorders10
Structure–Activity Relationship Study of 1H-Pyrrole-3-carbonitrile Derivatives as STING Receptor Agonists10
Selective Wee1 Inhibitors Led to Antitumor Activity In Vitro and Correlated with Myelosuppression10
Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors10
Issue Publication Information10
Steroid–Quinoline Hybrids for Disruption and Reversion of Protein Aggregation Processes10
Relevance of the Trillion-Sized Chemical Space “eXplore” as a Source for Drug Discovery9
Potent, Selective, and Orally Bioavailable Quinazoline-Based STK17A/B Dual Inhibitors9
NMR-Based Fragment Screen of the von Hippel-Lindau Elongin C&B Complex9
ACS Medicinal Chemistry Letters: An Innovation Ten Years in the Making9
Novel Aminocyclobutanes as Monoacylglycerol Lipase Modulators9
Novel 2-Pyrrolidone Derivatives as Negative Allosteric Modulators of GluN2B-Containing NMDA Receptors9
Engineering the Next Generation of Psychedelic Therapeutics through Serotonergic Precision and Pharmacokinetic Control9
Discovery of Novel Pyrimidine Derivatives as Human Pin1 Covalent Inhibitors9
Discovery of Kinesin KIF18A Inhibitor ATX020: Tactical Application of Silicon Atom Replacement9
Structure-Based Design of Novel TLR7/8 Agonist Payloads Enabling an Immunomodulatory Conjugate Approach9
Novel Lactams as Cbl-b Inhibitors for Treating Cancer9
9,10-Bis[(4-(2-hydroxyethyl)piperazine-1-yl)prop2-yne-1-yl]anthracene: G-Quadruplex Selectivity and Anticancer Activity9
Mining Druggable Sites in Influenza A Hemagglutinin: Binding of the Pinanamine-Based Inhibitor M0909
How a Blockchain Approach Can Improve Data Reliability in the COVID-19 Pandemic9
Discovery of Indole-Based PDE5 Inhibitors: Synthesis and Pharmacological Evaluation9
Discovery of INCB126503 as a Potent and Selective FGFR2/3 Inhibitor9
Design, Synthesis, and Biological Evaluation of Tetrazol-2-yl-acetamides as Novel Antitubercular Agents9
A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir9
A Neutral Flavin–Triphenylamine Probe for Mitochondrial Bioimaging under Different Microenvironments9
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2–p53 Inhibitor9
Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release9
Biological Effects of Modifications of the Englerin A Glycolate9
The Inhibitors of Mucosa-Associated Lymphoid Tissue Lymphoma Translocation Protein 1 (MALT-1) Protease as Potential Treatment of ABC-DLBCL and Similar Diseases9
Discovery of Selective Aldehyde Dehydrogenase Inhibitors for the Treatment of Cancer9
MALT1 Inhibitors for Treating Cancer and Immunological Diseases9
Inhibitors of Nav1.7 for the Treatment of Pain9
Discovery of Novel Hydroxyimine-Tethered Benzenesulfonamides as Potential Human Carbonic Anhydrase IX/XII Inhibitors9
Discovery of Non-Covalent Inhibitors for SARS-CoV-2 PLpro: Integrating Virtual Screening, Synthesis, and Experimental Validation9
Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries9
Optimization of Brain Penetrant SARM1 Orthosteric Inhibitors and Discovery of Their Paradoxical Subinhibitory Activation8
Application of Compositions Comprising a KRAS G12C Inhibitor and an EGFR Inhibitor for the Potential Treatment of Cancer8
Radiosynthesis and Preclinical Evaluation of a Carbon-11 Labeled Phosphodiesterase 7 Inhibitor for PET Neuroimaging8
In This Issue, Volume 15, Issue 48
Issue Publication Information8
Bicyclic Inhibitors of Branched-Chain α-Keto Acid Dehydrogenase Kinase (BDK) with In Vivo Activity8
A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors8
Ligand Design with Accelerated Disulfide Formation with Serum Albumin to Extend Blood Retention8
Innovations in Precision Oncology: Biomarker-Driven Approaches for Enhanced Cancer Therapy8
Insight on Some Newly Synthesized Trisubstituted Imidazolinones as VEGFR-2 Inhibitors8
Advances in the Quest for Safe and Effective Drugs That Target the Cannabinoid Receptor Type 1 (CB1)8
Exploring the 1-(4-Nitrophenyl)-3-arylprop-2-en-1-one Scaffold for the Selective Inhibition of Monoamine Oxidase B8
Structure–Activity Relationship of Anti-Mycobacterium abscessus Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors8
BTZ-Derived Benzisothiazolinones with In Vitro Activity against Mycobacterium tuberculosis8
Integrated Advancements in Neuroplasticity, Psychedelic Therapeutics, and AI-Driven Innovations for Precision Medicine8
Issue Publication Information8
Design and Assessment of First-Generation Heterobifunctional PPARα/STING Modulators8
Total Synthesis as Training for Medicinal Chemistry8
Novel Thienopyrrole Compounds for Treating Autoimmune Diseases and Inflammatory Conditions8
Call for Papers: Exploring the Use of AI/ML Technologies in Medicinal Chemistry and Drug Discovery8
Novel Bicyclic Heterocycles as MRGPRX2 Antagonists for Treating Inflammatory Diseases8
Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists8
Investigation of Isobactin Analogues of Teixobactin8
Development of Conformationally Restricted Negamycin Derivatives for Potent Readthrough Activity8
Issue Publication Information8
Identification of 5-Thiocyanatothiazol-2-amines Disrupting WDR5-MYC Protein–Protein Interactions8
Structural Evaluations of a Selective Human STINGA230 Agonist and Its Use in Macrophage Immunotherapies8
Novel AHR Agonists for Treating Psoriasis8
Issue Editorial Masthead8
Cytosolic Enzymes Generate Cannabinoid Metabolites 7-Carboxycannabidiol and 11-Nor-9-carboxytetrahydrocannabinol8
Novel Cyanotriazole Compounds for Treating Kinetoplastid Diseases, Particularly, Chagas Disease, Leishmaniasis, and Human African Trypanosomiasis8
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