ACS Medicinal Chemistry Letters

Article	Citations
Solution Conformations Shed Light on PROTAC Cell Permeability	106
Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation	62
Decarboxylative Cross-Coupling: A Radical Tool in Medicinal Chemistry	60
Steering New Drug Discovery Campaigns: Permeability, Solubility, and Physicochemical Properties in the bRo5 Chemical Space	55
Risdiplam, the First Approved Small Molecule Splicing Modifier Drug as a Blueprint for Future Transformative Medicines	51
The Growing Importance of Chirality in 3D Chemical Space Exploration and Modern Drug Discovery Approaches for Hit-ID	46
Design and Evaluation of Bispidine-Based SARS-CoV-2 Main Protease Inhibitors	44
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate	43
Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency	42
Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery	41
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia	41
Design, Synthesis, and Biological Evaluation of Imidazopyridines as PD-1/PD-L1 Antagonists	39
Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands	37
Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain	35
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation	30
Trisubstituted Pyrrolinones as Small-Molecule Inhibitors Disrupting the Protein–RNA Interaction of LIN28 and Let-7	30
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands	29
Discovery of the First Orally Available, Selective KNa1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series	29
Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens	29
SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression	28
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington’s Disease	28
Contemporary Computational Applications and Tools in Drug Discovery	28
Intriguing Antiviral Modified Nucleosides: A Retrospective View into the Future Treatment of COVID-19	28
Rational Control of Molecular Properties Is Mandatory to Exploit the Potential of PROTACs as Oral Drugs	27
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds	27

Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs	27
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1	26
A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir	26
Pilot Study to Quantify Palladium Impurities in Lead-like Compounds Following Commonly Used Purification Techniques	25
On the Selectivity of Heparan Sulfate Recognition by SARS-CoV-2 Spike Glycoprotein	25
BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate	25
Accelerating Drug Discovery: Synthesis of Complex Chemotypes via Multicomponent Reactions	24
Synthesis, Inhibitory Activity, and In Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core	24
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2	24
Contemporary Progress and Opportunities in RNA-Targeted Drug Discovery	23
2-Cyanoisonicotinamide Conjugation: A Facile Approach to Generate Potent Peptide Inhibitors of the Zika Virus Protease	23
mRNA Display Reaches for the Clinic with New PCSK9 Inhibitor	23
Design and Implementation of Synthetic RNA Binders for the Inhibition of miR-21 Biogenesis	23
Discovery of Investigational Drug CT1812, an Antagonist of the Sigma-2 Receptor Complex for Alzheimer’s Disease	23
Peripherally Crowded Cationic Phthalocyanines as Efficient Photosensitizers for Photodynamic Therapy	22
Identification of Potent Reverse Indazole Inhibitors for HPK1	22
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)	22
Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase	22
Recent Advances in Alchemical Binding Free Energy Calculations for Drug Discovery	22
Advancing New Chemical Modalities into Clinical Studies	21
Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay	21
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer	21
Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist	21
Development of Potent and Selective Janus Kinase 2/3 Directing PG–PROTACs	20
Promising Non-cytotoxic Monosubstituted Chalcones to Target Monoamine Oxidase-B	19
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors	19
A Green-Absorbing, Red-Fluorescent Phenalenone-Based Photosensitizer as a Theranostic Agent for Photodynamic Therapy	19
GPCR Inhibition in Treating Lymphoma	19
Conversion of a PROTAC Mutant Huntingtin Degrader into Small-Molecule Hydrophobic Tags Focusing on Drug-like Properties	19
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry	19
Phenyl Dihydrouracil: An Alternative Cereblon Binder for PROTAC Design	19
Determination of Slow-Binding HDAC Inhibitor Potency and Subclass Selectivity	19
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead	18
1,5-Disubstituted 1,2,3-Triazoles as Amide Bond Isosteres Yield Novel Tumor-Targeting Minigastrin Analogs	18
Cell Permeability of Isomeric Macrocycles: Predictions and NMR Studies	18
Discovery and Development of Cyclic Peptide Inhibitors of CIB1	18
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies	18
Dual Glycolate Oxidase/Lactate Dehydrogenase A Inhibitors for Primary Hyperoxaluria	18
Discovery of DS79932728: A Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease	17
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET	17
SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1	17
Development of Chimeric Molecules That Degrade the Estrogen Receptor Using Decoy Oligonucleotide Ligands	17
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors	17
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1	17
Physicochemistry of Cereblon Modulating Drugs Determines Pharmacokinetics and Disposition	17
Resorufin Enters the Photodynamic Therapy Arena: A Monoamine Oxidase Activatable Agent for Selective Cytotoxicity	17
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)	17
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins	17
Computer Prediction of pKa Values in Small Molecules and Proteins	17
Influence of 4′-Substitution on the Activity of Gemcitabine and Its ProTide Against VZV and SARS-CoV-2	16

Fragment Ligands of the m6A-RNA Reader YTHDF2	16
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448)	16
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin	16
Discovery of Small Molecule Entry Inhibitors Targeting the Fusion Peptide of SARS-CoV-2 Spike Protein	16
Synthesis of C6-Substituted Purine Nucleoside Analogues via Late-Stage Photoredox/Nickel Dual Catalytic Cross-Coupling	15
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use	15
Conjugation of a Blood Brain Barrier Peptide Shuttle to an Fc Domain for Brain Delivery of Therapeutic Biomolecules	15
Role of Fluorination in the Histone Deacetylase 6 (HDAC6) Selectivity of Benzohydroxamate-Based Inhibitors	15
Amide Tethered 4-Aminoquinoline-naphthalimide Hybrids: A New Class of Possible Dual Function Antiplasmodials	15
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field	15
Dual Reversible Coumarin Inhibitors Mutually Bound to Monoamine Oxidase B and Acetylcholinesterase Crystal Structures	15
Flavonol-Based Carbon Monoxide Delivery Molecule with Endoplasmic Reticulum, Mitochondria, And Lysosome Localization	15
Bioisostere Effects on the EPSA of Common Permeability-Limiting Groups	14
Antivirals against (Re)emerging Flaviviruses: Should We Target the Virus or the Host?	14
Semisynthetic Derivatives of the Verticillin Class of Natural Products through Acylation of the C11 Hydroxy Group	14
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay	14
Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors	14
Ugi Reaction Synthesis of Oxindole–Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors	14
Accelerated Discovery of Macrocyclic CDK2 Inhibitor QR-6401 by Generative Models and Structure-Based Drug Design	14
Large-Scale Screening of Antifungal Peptides Based on Quantitative Structure–Activity Relationship	14
Macrocyclic Peptides as a Novel Class of NNMT Inhibitors: A SAR Study Aimed at Inhibitory Activity in the Cell	14
Site-specific Incorporation of 2′,5′-Linked Nucleic Acids Enhances Therapeutic Profile of Antisense Oligonucleotides	13
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity	13
Latest Research Trends in Agrochemical Fungicides: Any Learnings for Pharmaceutical Antifungals?	13
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction	13
Design, Synthesis, and Evaluation of PD-1/PD-L1 Antagonists Bearing a Benzamide Scaffold	13
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFRT790M/C797S Mutants	13
Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein	13
Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group	13
ChemBeads-Enabled Photoredox High-Throughput Experimentation Platform to Improve C(sp2)–C(sp3) Decarboxylative Couplings	13
Fueling the Pipeline via Innovations in Organic Synthesis	13
Identification, Synthesis, and Characterization of a Major Circulating Human Metabolite of TRPV4 Antagonist GSK2798745	13
Thiol- and Disulfide-Containing Vancomycin Derivatives Against Bacterial Resistance and Biofilm Formation	13
Structurally Optimized Potent Dual-Targeting NBTI Antibacterials with an Enhanced Bifurcated Halogen-Bonding Propensity	13
Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation	13
Novel Small Molecule RNA m6A Demethylase AlkBH5 Inhibitors for Treating Cancer	13
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators	13
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach	13
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow	13
Biological Evaluation of 5′-(N-Ethylcarboxamido)adenosine Analogues as Grp94-Selective Inhibitors	13
Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity	13
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors	13
A New Highly Deuterated [18F]AV-45, [18F]D15FSP, for Imaging β-Amyloid Plaques in the Brain	13
Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones Active against Plasmodium and Trypanosomatids	13
Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor	12
Efficient NMR Screening Approach to Discover Small Molecule Fragments Binding Structured RNA	12
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor	12
Novel Histone Deacetylase 6 Inhibitors for Treating Alzheimer’s Disease and Cancer	12
Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication	12
BRD9 Bifunctional Degraders for Treating Cancer	12
Virtual Screening Approach to Identifying a Novel and Tractable Series ofPseudomonas aeruginosaElastase Inhibitors	12
Discovery of Antibacterial Contezolid Acefosamil: Innovative O-Acyl Phosphoramidate Prodrug for IV and Oral Therapies	12
Novel Nitrile Peptidomimetics for Treating COVID-19	12
“I’ll Be Back”: The Resurrection of Dezocine	12
Novel Copper(II) Complex with a 4-Acylpyrazolone Derivative and Coligand Induce Apoptosis in Liver Cancer Cells	12
A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists	12
Novel Histone Acetyltransferase (HAT) Inhibitors for Treating Diseases	12
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology	12
Structural Characterization of Thiadiazolesulfonamide Inhibitors Bound to Neisseria gonorrhoeae α-Carbonic Anhydrase	12
Evaluation of 1,3,4-Thiadiazole Carbonic Anhydrase Inhibitors for Gut Decolonization of Vancomycin-Resistant Enterococci	12
Novel Isoindolinone-Based Analogs of the Natural Cyclic Peptide Fenestin A: Synthesis and Antitumor Activity	12
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2	12
Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies	12
Exploration of a 14-3-3 PPI Pocket by Covalent Fragments as Stabilizers	12
N-Aromatic-Substituted Indazole Derivatives as Brain-Penetrant and Orally Bioavailable JNK3 Inhibitors	12
Relevance of the Trillion-Sized Chemical Space “eXplore” as a Source for Drug Discovery	12
Discovery of a Series of Pyrazinone RORγ Antagonists and Identification of the Clinical Candidate BI 730357	12
Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors	11
Discovery of Potent Inhibitors of Streptococcus mutans Biofilm with Antivirulence Activity	11
Novel Thienopyridines as RIPK2 Inhibitors for Treating Inflammatory Bowel Disease	11
Interaction Studies between Carbonic Anhydrase and a Sulfonamide Inhibitor by Experimental and Theoretical Approaches	11
Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids	11
Pyridine-Based 1,2,4-Triazolo-Tethered Indole Conjugates Potentially Affecting TNKS and PI3K in Colorectal Cancer	11
Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties	11
Hydrophobic Tagging-Induced Degradation of PDEδ in Colon Cancer Cells	11
Discovery of First-in-Class Small Molecule Inhibitors of Lymphocyte Activation Gene 3 (LAG-3)	11
Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3	11
The Compelling Demand for an Effective PrPC-Directed Therapy against Prion Diseases	11
Identification of RAD51–BRCA2 Inhibitors Using N-Acylhydrazone-Based Dynamic Combinatorial Chemistry	11
Development of Urea-Bond-Containing Michael Acceptors as Antitrypanosomal Agents Targeting Rhodesain	11

Amide–Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility	11
Structure–Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors	11
Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2	11
In Silico Targeting of the Long Noncoding RNA MALAT1	11
Discovery of a Potent and Selective Covalent p300/CBP Inhibitor	11
Porphyrin-Based Tumor-Targeting Theranostic Agent: Gd-TDAP	11
Novel Linker Variants of Antileishmanial/Antitubercular 7-Substituted 2-Nitroimidazooxazines Offer Enhanced Solubility	11
Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation	11
Small Molecule Inhibitors of TET Dioxygenases: Bobcat339 Activity Is Mediated by Contaminating Copper(II)	11
Discovery of Surfactins as Inhibitors of MicroRNA Processing Using Cat-ELCCA	11
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors	11
Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors	11
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum	11
Highly Potent and Oral Macrocyclic Peptides as a HIV-1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization	11
Development of Potent 3-Br-isoxazoline-Based Antimalarial and Antileishmanial Compounds	10
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1	10
Turning a Quinoline-based Steroidal Anticancer Agent into Fluorescent Dye for its Tracking by Cell Imaging	10
Inhibition of Thiamine Diphosphate-Dependent Enzymes by Triazole-Based Thiamine Analogues	10
2-Trifluoromethylthiazole-5-carboxamides: Analogues of a Stilbene-Based Anti-HIV Agent that Impact HIV mRNA Processing	10
Identification and Evaluation of Brominated Carbazoles as a Novel Antibiotic Adjuvant Scaffold in MRSA	10
Sigma-1 and Sigma-2 Receptor Modulators as Potential Therapeutics for Alzheimer’s Disease	10
Novel PRMT5 Inhibitors for Treating Cancer	10
Antibacterial Nanoassembled Calix[4]arene Exposing Choline Units Inhibits Biofilm and Motility of Gram Negative Bacteria	10
Design and Synthesis of Tranylcypromine-Derived LSD1 Inhibitors with Improved hERG and Microsomal Stability Profiles	10
Discovery and Preclinical Profiling of GSK3839919, a Potent HIV-1 Allosteric Integrase Inhibitor	10
Development of Myostatin Inhibitory d-Peptides to Enhance the Potency, Increasing Skeletal Muscle Mass in Mice	10
Discovery of Desmuramylpeptide NOD2 Agonists with Single-Digit Nanomolar Potency	10
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors	10
Lathyrane Diterpenoids as Novel hPXR Agonists: Isolation, Structural Modification, and Structure–Activity Relationships	10
Design, Synthesis, and Bioevaluation of Pyrido[2,3-d]pyrimidin-7-ones as Potent SOS1 Inhibitors	10
Steroid–Quinoline Hybrids for Disruption and Reversion of Protein Aggregation Processes	10
Design and Synthesis of Oleanolic Acid Trimers to Enhance Inhibition of Influenza Virus Entry	10
C20-nor-Abietane and Three Abietane Diterpenoids from Plectranthus mutabilis Leaves as P-Glycoprotein Modulators	10
Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents	10
Improvement of Photodynamic Activity by a Stable System Consisting of a C60 Derivative and Photoantenna in Liposomes	10
Synthesis and Biological Evaluation of Aurachin D Analogues as Inhibitors of Mycobacterium tuberculosis Cytochrome bd Oxidase	10
Discovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na+/H+ Exchanger Isoform 3	10
Novel 2-Aryloxazoline Compounds Exhibit an Inhibitory Effect on Candida spp., Including Antifungal-Resistant Isolates	10
Synthesis of Resolvin E1 and Its Conformationally Restricted Cyclopropane Congeners with Potent Anti-Inflammatory Effect	10
Escaping from Flatland: Antimalarial Activity of sp3-Rich Bridged Pyrrolidine Derivatives	10
Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B	10
A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors	10
Discovery of a Novel Series of Imidazopyrazine Derivatives as Potent SHP2 Allosteric Inhibitors	10
Discovery and Nanosized Preparations of (S,R)-Tylophorine Malate as Novel anti-SARS-CoV-2 Agents	9
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205	9
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors	9
LipMetE (Lipophilic Metabolism Efficiency) as a Simple Guide for Half-Life and Dosing Regimen Prediction of Oral Drugs	9
Discovery of Coumarin-Based MEK1/2 PROTAC Effective in Human Cancer Cells	9
Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures	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
Novel Substituted Tetrazoles as ACSS2 Inhibitors for Treating Cancer	9
Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site	9
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy	9
The Hitchhiker’s Guide to Deep Learning Driven Generative Chemistry	9
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides	9
Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors	9
Discovery of Novel Aldo-Keto Reductase 1C3 Inhibitors as Chemotherapeutic Potentiators for Cancer Drug Resistance	9
Derivatization Design of Synthetically Accessible Space for Optimization: In Silico Synthesis vs Deep Generative Design	9
Inactivators of Ornithine Aminotransferase for the Treatment of Hepatocellular Carcinoma	9
Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity	9
A New FXR Ligand Chemotype with Agonist/Antagonist Switch	9
Photoaffinity Probe Reveals the Potential Target of Harringtonolide for Cancer Cell Migration Inhibition	9
Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors	9
Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors	9
Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors	9
Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity	9
Discovery of Novel Small-Molecule FAK Activators Promoting Mucosal Healing	8
Structure–Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro	8
Discovery of Novel Hydroxyimine-Tethered Benzenesulfonamides as Potential Human Carbonic Anhydrase IX/XII Inhibitors	8
Discovery of a Positron Emission Tomography Radiotracer Selectively Targeting the BD1 Bromodomains of BET Proteins	8
Synthesis and Metabolism of BTN3A1 Ligands: Studies on Diene Modifications to the Phosphoantigen Scaffold	8
Design and Structure–Activity Relationship of a Potent Furin Inhibitor Derived from Influenza Hemagglutinin	8
Tricyclic Carboxamide Derivatives as PRMT5 Inhibitors for Treating Cancer	8
Identification of gp120 Residue His105 as a Novel Target for HIV-1 Neutralization by Small-Molecule CD4-Mimics	8
Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist	8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline	8
Small-Molecule Inhibitors of the MLL1 CXXC Domain, an Epigenetic Reader of DNA Methylation	8
Fragment-Based Discovery of Novel Allosteric MEK1 Binders	8
S-Protected Cysteine Sulfoxide-Enabled Tryptophan-Selective Modification with Application to Peptide Lipidation	8
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA	8
Space Medicines for Space Health	8
Positional Isomers of Biphenyl Antimicrobial Peptidomimetic Amphiphiles	8
Novel Bromodomain BRD4 Inhibitors for Treating Cancer	8
The Inhibitors of Protein Tyrosine Phosphatase Nonreceptor Type 2 (PTPN2) as Potential Enhancers of Cancer Immunotherapy and Type 1 (PTPN1) as Treatment of Metabolic Diseases	8
Dodecaborate Conjugates Targeting Tumor Cell Overexpressing Translocator Protein for Boron Neutron Capture Therapy	8
The Quest for Oral PROTAC drugs: Evaluating the Weaknesses of the Screening Pipeline	8
Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity	8
Structure–Activity Relationship Study of Tertiary Alcohol Hsp90α-Selective Inhibitors with Novel Binding Mode	8
Nanoacetylated N-(4-Hydroxyphenyl) Retinamide Modulates Histone Acetylation–Methylation Epigenetic Disparity to Restrict Epithelial–Mesenchymal Transition in Neuroblastoma	8
Development of Polyamine Lassos as Polyamine Transport Inhibitors	8
Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20	8
Aroylhydrazone Glycoconjugate Prochelators Exploit Glucose Transporter 1 (GLUT1) to Target Iron in Cancer Cells	8
Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1–Nrf2 PPI Inhibitor	8
Discovery of a Lead Compound for Specific Inhibition of Type I Collagen Production in Fibrosis	8