ACS Medicinal Chemistry Letters

Article	Citations
Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2	168
Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment	139
Solution Conformations Shed Light on PROTAC Cell Permeability	95
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs	80
Visible-Light Photocatalysis as an Enabling Technology for Drug Discovery: A Paradigm Shift for Chemical Reactivity	67
The Advent of Generative Chemistry	65
Structural Impact of Mutation D614G in SARS-CoV-2 Spike Protein: Enhanced Infectivity and Therapeutic Opportunity	61
A Role for Metal-Based Drugs in Fighting COVID-19 Infection? The Case of Auranofin	53
Steering New Drug Discovery Campaigns: Permeability, Solubility, and Physicochemical Properties in the bRo5 Chemical Space	51
Ultra-High-Throughput Acoustic Droplet Ejection-Open Port Interface-Mass Spectrometry for Parallel Medicinal Chemistry	47
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation	47
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors	46
Biotransformation: Impact and Application of Metabolism in Drug Discovery	45
Decarboxylative Cross-Coupling: A Radical Tool in Medicinal Chemistry	41
Risdiplam, the First Approved Small Molecule Splicing Modifier Drug as a Blueprint for Future Transformative Medicines	41
Evaluation of 3-Dimensionality in Approved and Experimental Drug Space	41
Systematic Investigation of the Permeability of Androgen Receptor PROTACs	41
Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency	39
The Growing Importance of Chirality in 3D Chemical Space Exploration and Modern Drug Discovery Approaches for Hit-ID	38
Design and Evaluation of Bispidine-Based SARS-CoV-2 Main Protease Inhibitors	38
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate	36
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging	32
Design, Synthesis, and Biological Evaluation of Imidazopyridines as PD-1/PD-L1 Antagonists	32
Simultaneous Inhibition of SIRT2 Deacetylase and Defatty-Acylase Activities via a PROTAC Strategy	31
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5)	30

Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain	29
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia	29
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies	28
Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands	27
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands	27
Establishing the Structure–Activity Relationship of Daptomycin	27
Blocking Coronavirus 19 Infection via the SARS-CoV-2 Spike Protein: Initial Steps	27
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group	26
Emerging Chromatography-Free High-Throughput Mass Spectrometry Technologies for Generating Hits and Leads	26
Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models	26
Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae	25
Discovery of Dotinurad (FYU-981), a New Phenol Derivative with Highly Potent Uric Acid Lowering Activity	25
Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs	25
SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression	24
Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens	24
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation	24
Intriguing Antiviral Modified Nucleosides: A Retrospective View into the Future Treatment of COVID-19	24
Trisubstituted Pyrrolinones as Small-Molecule Inhibitors Disrupting the Protein–RNA Interaction of LIN28 and Let-7	24
On the Selectivity of Heparan Sulfate Recognition by SARS-CoV-2 Spike Glycoprotein	24
Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9)	24
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington’s Disease	23
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs	23
A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir	23
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation	23
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family	23
Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery	22
Discovery of the First Orally Available, Selective KNa1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series	22
Peripherally Crowded Cationic Phthalocyanines as Efficient Photosensitizers for Photodynamic Therapy	22
2-Cyanoisonicotinamide Conjugation: A Facile Approach to Generate Potent Peptide Inhibitors of the Zika Virus Protease	21
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors	21
De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits	21
Discovery of Investigational Drug CT1812, an Antagonist of the Sigma-2 Receptor Complex for Alzheimer’s Disease	20
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance	20
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1	20
Chemical Modification of Linkers Provides Stable Linker–Payloads for the Generation of Antibody–Drug Conjugates	20
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds	19
Contemporary Computational Applications and Tools in Drug Discovery	19
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2	19
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer	19
GPCR Inhibition in Treating Lymphoma	19
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer	19
ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model	18
Pilot Study to Quantify Palladium Impurities in Lead-like Compounds Following Commonly Used Purification Techniques	18
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive Staphylococcus aureus	18
2-Aminooxazole as a Novel Privileged Scaffold in Antitubercular Medicinal Chemistry	18
Novel Betulinic Acid–Nucleoside Hybrids with Potent Anti-HIV Activity	18
Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist	18
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)	18
Structural Approach to Assessing the Innovativeness of New Drugs Finds Accelerating Rate of Innovation	18
Design and Implementation of Synthetic RNA Binders for the Inhibition of miR-21 Biogenesis	18

Development of Potent and Selective Janus Kinase 2/3 Directing PG–PROTACs	17
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors	17
mRNA Display Reaches for the Clinic with New PCSK9 Inhibitor	17
Design, Synthesis, and Biological Evaluation of Novel Acylhydrazone Derivatives as Potent Neuraminidase Inhibitors	17
Development of Chimeric Molecules That Degrade the Estrogen Receptor Using Decoy Oligonucleotide Ligands	17
Resorufin Enters the Photodynamic Therapy Arena: A Monoamine Oxidase Activatable Agent for Selective Cytotoxicity	17
Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation	17
Cell Permeability of Isomeric Macrocycles: Predictions and NMR Studies	17
Antiferroptotic Activity of Phenothiazine Analogues: A Novel Therapeutic Strategy for Oxidative Stress Related Disease	17
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate	17
Identification of Potent Reverse Indazole Inhibitors for HPK1	17
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors	17
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)	16
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1	16
Discovery of Small Molecule Entry Inhibitors Targeting the Fusion Peptide of SARS-CoV-2 Spike Protein	16
Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay	16
Promising Non-cytotoxic Monosubstituted Chalcones to Target Monoamine Oxidase-B	16
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition	16
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors	16
Synthesis, Inhibitory Activity, and In Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core	16
Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition	16
Design and Synthesis of 1,2-Deoxy-pyranose Derivatives of Spliceostatin A toward Prostate Cancer Treatment	16
Influence of 4′-Substitution on the Activity of Gemcitabine and Its ProTide Against VZV and SARS-CoV-2	16
Challenges and Opportunities for Drug Discovery in Developing Countries: The Example of Cutaneous Leishmaniasis	16
Discovery of Tricyclic Xanthines as Agonists of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18	16
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin	15
Toward the Target: Tilorone, Quinacrine, and Pyronaridine Bind to Ebola Virus Glycoprotein	15
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead	15
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors	15
Amide Tethered 4-Aminoquinoline-naphthalimide Hybrids: A New Class of Possible Dual Function Antiplasmodials	15
Contemporary Progress and Opportunities in RNA-Targeted Drug Discovery	14
Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells	14
Antivirals against (Re)emerging Flaviviruses: Should We Target the Virus or the Host?	14
Synthesis of C6-Substituted Purine Nucleoside Analogues via Late-Stage Photoredox/Nickel Dual Catalytic Cross-Coupling	14
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode	14
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies	14
Semisynthetic Analogs of the Antibiotic Fidaxomicin—Design, Synthesis, and Biological Evaluation	14
A Green-Absorbing, Red-Fluorescent Phenalenone-Based Photosensitizer as a Theranostic Agent for Photodynamic Therapy	14
Discovery and Development of Cyclic Peptide Inhibitors of CIB1	14
Virtual Screening for Ligand Discovery at the σ1 Receptor	14
Computer Prediction of pKa Values in Small Molecules and Proteins	14
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry	14
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET	14
Advancing New Chemical Modalities into Clinical Studies	14
1,5-Disubstituted 1,2,3-Triazoles as Amide Bond Isosteres Yield Novel Tumor-Targeting Minigastrin Analogs	14
Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity	13
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia	13
Bioisostere Effects on the EPSA of Common Permeability-Limiting Groups	13
Bromocriptine as a Novel Pharmacological Chaperone for Mucopolysaccharidosis IV A	13
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay	13
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin	13
Dual Glycolate Oxidase/Lactate Dehydrogenase A Inhibitors for Primary Hyperoxaluria	13
meso-Thiophenium Porphyrins and Their Zn(II) Complexes: A New Category of Cationic Photosensitizers	13
Thiol- and Disulfide-Containing Vancomycin Derivatives Against Bacterial Resistance and Biofilm Formation	13
Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation	13
Ugi Reaction Synthesis of Oxindole–Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors	13
Dual Reversible Coumarin Inhibitors Mutually Bound to Monoamine Oxidase B and Acetylcholinesterase Crystal Structures	13
Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders	13
Conjugation of a Blood Brain Barrier Peptide Shuttle to an Fc Domain for Brain Delivery of Therapeutic Biomolecules	13
Discovery of DS79932728: A Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease	13
Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3Kγ Inhibitors	13
Semisynthetic Derivatives of the Verticillin Class of Natural Products through Acylation of the C11 Hydroxy Group	13
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity	13
Site-specific Incorporation of 2′,5′-Linked Nucleic Acids Enhances Therapeutic Profile of Antisense Oligonucleotides	13
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)	12
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach	12
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins	12
Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase	12
Automation of Synthesis in Medicinal Chemistry: Progress and Challenges	12
Design, Synthesis, and Evaluation of PD-1/PD-L1 Antagonists Bearing a Benzamide Scaffold	12
Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell	12
Novel Copper(II) Complex with a 4-Acylpyrazolone Derivative and Coligand Induce Apoptosis in Liver Cancer Cells	12
Role of Fluorination in the Histone Deacetylase 6 (HDAC6) Selectivity of Benzohydroxamate-Based Inhibitors	12
Conversion of a PROTAC Mutant Huntingtin Degrader into Small-Molecule Hydrophobic Tags Focusing on Drug-like Properties	12
Fueling the Pipeline via Innovations in Organic Synthesis	12
Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity	12
Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357	12
Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group	12
Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor	12
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity	12

SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1	12
Synthesis and Evaluation of Ginkgolic Acid Derivatives as SUMOylation Inhibitors	12
Recent Advances in Alchemical Binding Free Energy Calculations for Drug Discovery	12
Discovery of Adamantane Carboxamides as Ebola Virus Cell Entry and Glycoprotein Inhibitors	12
Accelerating Drug Discovery: Synthesis of Complex Chemotypes via Multicomponent Reactions	11
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators	11
Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome	11
Novel Histone Deacetylase 6 Inhibitors for Treating Alzheimer’s Disease and Cancer	11
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology	11
Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35	11
Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation	11
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma	11
Relevance of the Trillion-Sized Chemical Space “eXplore” as a Source for Drug Discovery	11
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction	11
Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies	11
Phenyl Dihydrouracil: An Alternative Cereblon Binder for PROTAC Design	11
Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones Active against Plasmodium and Trypanosomatids	11
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors	11
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors	11
N-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors	11
Novel Histone Acetyltransferase (HAT) Inhibitors for Treating Diseases	11
Biological Evaluation of 5′-(N-Ethylcarboxamido)adenosine Analogues as Grp94-Selective Inhibitors	11
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin	11
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow	11
A New Highly Deuterated [18F]AV-45, [18F]D15FSP, for Imaging β-Amyloid Plaques in the Brain	11
Novel Thienopyridines as RIPK2 Inhibitors for Treating Inflammatory Bowel Disease	11
Novel Isoindolinone-Based Analogs of the Natural Cyclic Peptide Fenestin A: Synthesis and Antitumor Activity	11
Discovery of Surfactins as Inhibitors of MicroRNA Processing Using Cat-ELCCA	11
Novel Nitrile Peptidomimetics for Treating COVID-19	11
Identification of Novel Rho-Kinase-II Inhibitors with Vasodilatory Activity	11
BRD9 Bifunctional Degraders for Treating Cancer	11
Polysaccharide-Based Nanoparticles for Two-Step Responsive Release of Antitumor Drug	11
Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β	11
Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication	11
Covalent Bridging of Corilagin Improves Antiferroptosis Activity: Comparison with 1,3,6-Tri-O-galloyl-β-d-glucopyranose	11
Conjugation Ratio, Light Dose, and pH Affect the Stability of Panitumumab–IR700 for Near-Infrared Photoimmunotherapy	11
Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties	10
Dual-Target Inhibitors of the Folate Pathway Inhibit Intrinsically Trimethoprim-Resistant DfrB Dihydrofolate Reductases	10
Fluorescent Probes for Ecto-5′-nucleotidase (CD73)	10
Hydrophobic Tagging-Induced Degradation of PDEδ in Colon Cancer Cells	10
Discovery of a Potent and Selective Covalent p300/CBP Inhibitor	10
A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists	10
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1	10
SMARCA2/4 PROTAC for Targeted Protein Degradation and Cancer Therapy	10
Structurally Optimized Potent Dual-Targeting NBTI Antibacterials with an Enhanced Bifurcated Halogen-Bonding Propensity	10
Discovery of Potent Inhibitors of Streptococcus mutans Biofilm with Antivirulence Activity	10
Lathyrane Diterpenoids as Novel hPXR Agonists: Isolation, Structural Modification, and Structure–Activity Relationships	10
Novel Small Molecule RNA m6A Demethylase AlkBH5 Inhibitors for Treating Cancer	10
Large-Scale Screening of Antifungal Peptides Based on Quantitative Structure–Activity Relationship	10
Mining Public Domain Data to Develop Selective DYRK1A Inhibitors	10
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors	10
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum	10
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity	10
Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors	10
Flavonol-Based Carbon Monoxide Delivery Molecule with Endoplasmic Reticulum, Mitochondria, And Lysosome Localization	10
Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745	10
Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2	10
The Compelling Demand for an Effective PrPC-Directed Therapy against Prion Diseases	10
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation	10
Pyridine-Based 1,2,4-Triazolo-Tethered Indole Conjugates Potentially Affecting TNKS and PI3K in Colorectal Cancer	10
2-Trifluoromethylthiazole-5-carboxamides: Analogues of a Stilbene-Based Anti-HIV Agent that Impact HIV mRNA Processing	10
Escaping from Flatland: Antimalarial Activity of sp3-Rich Bridged Pyrrolidine Derivatives	10
Vinyl Sulfone-Based Inhibitors of Nonstructural Protein 2 Block the Replication of Venezuelan Equine Encephalitis Virus	10
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor	10
Exploration of a 14-3-3 PPI Pocket by Covalent Fragments as Stabilizers	10
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use	10
Virtual Screening Approach to Identifying a Novel and Tractable Series of Pseudomonas aeruginosa Elastase Inhibitors	10
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7 Positive Allosteric Modulator Tool Compound	10
Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors	10
In Silico Targeting of the Long Noncoding RNA MALAT1	10
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors	10
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field	10
Development of Urea-Bond-Containing Michael Acceptors as Antitrypanosomal Agents Targeting Rhodesain	10
Amide–Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility	10
Discovery and SAR of Novel Disubstituted Quinazolines as Dual PI3Kalpha/mTOR Inhibitors Targeting Breast Cancer	9
Fragment Ligands of the m6A-RNA Reader YTHDF2	9
Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity	9
Derivatization Design of Synthetically Accessible Space for Optimization: In Silico Synthesis vs Deep Generative Design	9
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy	9
Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor	9
Novel 2-Aryloxazoline Compounds Exhibit an Inhibitory Effect on Candida spp., Including Antifungal-Resistant Isolates	9
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides	9
Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies	9
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile	9
Reducing the Toxicity of Designer Aminoglycosides as Nonsense Mutation Readthrough Agents for Therapeutic Targets	9
Efficient NMR Screening Approach to Discover Small Molecule Fragments Binding Structured RNA	9
Synthesis and Evaluation of Neutral Phosphate Triester Backbone-Modified siRNAs	9
Design and Synthesis of Oleanolic Acid Trimers to Enhance Inhibition of Influenza Virus Entry	9
Structure–Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors	9
Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors	9
Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors	9
Design and Synthesis of Tranylcypromine-Derived LSD1 Inhibitors with Improved hERG and Microsomal Stability Profiles	9
Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids	9
Identification and Evaluation of Brominated Carbazoles as a Novel Antibiotic Adjuvant Scaffold in MRSA	9
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors	9