SLAS Discovery

Article	Citations
E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones	148
RNA-Dependent RNA Polymerase as a Target for COVID-19 Drug Discovery	119
Targeting RNA with Small Molecules: Identification of Selective, RNA-Binding Small Molecules Occupying Drug-Like Chemical Space	64
Advances in Antibody–Drug Conjugate Design: Current Clinical Landscape and Future Innovations	48
Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors	48
A Critical and Concise Review of Mass Spectrometry Applied to Imaging in Drug Discovery	40
MALDI-TOF Mass Spectrometry-Based High-Throughput Screening for Inhibitors of the Cytosolic DNA Sensor cGAS	38
High-Throughput Screening for Drugs That Inhibit Papain-Like Protease in SARS-CoV-2	38
Comparison of Cell and Organoid-Level Analysis of Patient-Derived 3D Organoids to Evaluate Tumor Cell Growth Dynamics and Drug Response	36
Cryo-EM: The Resolution Revolution and Drug Discovery	35
Phenotypic Profiling of Reference Chemicals across Biologically Diverse Cell Types Using the Cell Painting Assay	32
High-Throughput Mass Spectrometry for Hit Identification: Current Landscape and Future Perspectives	32
Recommended Guidelines for Developing, Qualifying, and Implementing Complex In Vitro Models (CIVMs) for Drug Discovery	32
Discovery of Drug-Like Ligands for the Mac1 Domain of SARS-CoV-2 Nsp3	29
High-Throughput Imaging Assay for Drug Screening of 3D Prostate Cancer Organoids	29
A Mass Spectrometric Assay of METTL3/METTL14 Methyltransferase Activity	28
Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry	28
Acoustic Ejection Mass Spectrometry: A Fully Automatable Technology for High-Throughput Screening in Drug Discovery	25
Selecting Approaches for Hit Identification and Increasing Options by Building the Efficient Discovery of Actionable Chemical Matter from DNA-Encoded Libraries	24
A Review of the Preclinical and Clinical Efficacy of Remdesivir, Hydroxychloroquine, and Lopinavir-Ritonavir Treatments against COVID-19	24
Identification of Compounds for Butyrylcholinesterase Inhibition	24
Target-Directed Approaches for Screening Small Molecules against RNA Targets	22
Target Validation Using PROTACs: Applying the Four Pillars Framework	22
High-Content Phenotypic Profiling in Esophageal Adenocarcinoma Identifies Selectively Active Pharmacological Classes of Drugs for Repurposing and Chemical Starting Points for Novel Drug Discovery	21
A High-Throughput RNA Displacement Assay for Screening SARS-CoV-2 nsp10-nsp16 Complex toward Developing Therapeutics for COVID-19	21

Changing the HTS Paradigm: AI-Driven Iterative Screening for Hit Finding	21
CDK Family PROTAC Profiling Reveals Distinct Kinetic Responses and Cell Cycle–Dependent Degradation of CDK2	20
A Tale of Two Tails: Efficient Profiling of Protein Degraders by Specific Functional and Target Engagement Readouts	20
Repurposing Nimesulide, a Potent Inhibitor of the B0AT1 Subunit of the SARS-CoV-2 Receptor, as a Therapeutic Adjuvant of COVID-19	19
A High-Throughput Radioactivity-Based Assay for Screening SARS-CoV-2 nsp10-nsp16 Complex	19
High-Throughput Quantitative Assay Technologies for Accelerating the Discovery and Optimization of Targeted Protein Degradation Therapeutics	19
A Framework for Optimizing High-Content Imaging of 3D Models for Drug Discovery	19
Discovery of SARS-CoV-2 main protease covalent inhibitors from a DNA-encoded library selection	18
Identification of potent small molecule inhibitors of SARS-CoV-2 entry	18
Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes	18
Application of High-Throughput Automated Patch-Clamp Electrophysiology to Study Voltage-Gated Ion Channel Function in Primary Cortical Cultures	17
Using chemical and biological data to predict drug toxicity	17
Exploring the Lower Limit of Individual DNA-Encoded Library Molecules in Selection	17
Applied Biophysical Methods in Fragment-Based Drug Discovery	17
Public-Private Partnerships: Compound and Data Sharing in Drug Discovery and Development	17
Label-Free Screening of SARS-CoV-2 NSP14 Exonuclease Activity Using SAMDI Mass Spectrometry	16
Evaluating Very Deep Convolutional Neural Networks for Nucleus Segmentation from Brightfield Cell Microscopy Images	16
Validating ADME QSAR Models Using Marketed Drugs	16
MALDI-TOF-Based Affinity Selection Mass Spectrometry for Automated Screening of Protein–Ligand Interactions at High Throughput	16
Small-Molecule Degraders beyond PROTACs—Challenges and Opportunities	16
Lead identification using 3D models of pancreatic cancer	16
A high throughput screening assay for inhibitors of SARS-CoV-2 pseudotyped particle entry	15
A 3D Heterotypic Multicellular Tumor Spheroid Assay Platform to Discriminate Drug Effects on Stroma versus Cancer Cells	15
Comparative Analysis of Multiple Immunoassays for Cytokine Profiling in Drug Discovery	15
ASCT1 and ASCT2: Brother and Sister?	15
Development of High-Throughput Assays for Evaluation of Hematopoietic Progenitor Kinase 1 Inhibitors	14
CRISPR Meets Zebrafish: Accelerating the Discovery of New Therapeutic Targets	14
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening	14
Comparison of Approaches for Determining Bioactivity Hits from High-Dimensional Profiling Data	14
Secretome-Based Screening in Target Discovery	14
Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators	14
Z’ Does Not Need to Be > 0.5	14
Arrayed CRISPR Screening Identifies Novel Targets That Enhance the Productive Delivery of mRNA by MC3-Based Lipid Nanoparticles	14
Advanced High-Content-Screening Applications of Clonogenicity in Cancer	13
Efficiency Improvements and Discovery of New Substrates for a SARS-CoV-2 Main Protease FRET Assay	13
The Problems of Applying Classical Pharmacology Analysis to Modern In Vitro Drug Discovery Assays: Slow Binding Kinetics and High Target Concentration	13
A Scalable Approach Reveals Functional Responses of iPSC Cardiomyocyte 3D Spheroids	13
Maximizing the Value of Cancer Drug Screening in Multicellular Tumor Spheroid Cultures: A Case Study in Five Head and Neck Squamous Cell Carcinoma Cell Lines	13
A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination	13
Brief Guide: Experimental Strategies for High-Quality Hit Selection from Small-Molecule Screening Campaigns	12
Combining Supervised and Unsupervised Machine Learning Methods for Phenotypic Functional Genomics Screening	12
COMPARE Analysis, a Bioinformatic Approach to Accelerate Drug Repurposing against Covid-19 and Other Emerging Epidemics	12
In Vitro three-dimensional (3D) cell culture tools for spheroid and organoid models	12
waveRAPID—A Robust Assay for High-Throughput Kinetic Screens with the Creoptix WAVEsystem	12
The Impact of Variable Selection Coverage on Detection of Ligands from a DNA-Encoded Library Screen	12
CRISPR: A Screener’s Guide	11
HighVia—A Flexible Live-Cell High-Content Screening Pipeline to Assess Cellular Toxicity	11
Activity-Based Screening Assay for Mono-ADP-Ribosylhydrolases	11
Optimization of a Colorimetric Assay to Determine Lactate Dehydrogenase B Activity Using Design of Experiments	11
A Pilot Screen of a Novel Peptide Hormone Library Identified Candidate GPR83 Ligands	11

The Vital Role of Proteomics in Characterizing Novel Protein Degraders	11
CETSA MS Profiling for a Comparative Assessment of FDA-Approved Antivirals Repurposed for COVID-19 Therapy Identifies TRIP13 as a Remdesivir Off-Target	10
Development of a Cell-Based Immunodetection Assay for Simultaneous Screening of Antiviral Compounds Inhibiting Zika and Dengue Virus Replication	10
Identification of a Triple Drug Combination That Is Synergistically Cytotoxic for Triple-Negative Breast Cancer Cells Using a Novel Combination Discovery Approach	10
Detection and impact of hypoxic regions in multicellular tumor spheroid cultures formed by head and neck squamous cell carcinoma cells lines	10
Ion Channels and Relevant Drug Screening Approaches	10
Direct Comparison of Label-Free Biosensor Binding Kinetics Obtained on the Biacore 8K and the Carterra LSA	10
deepOrganoid: A brightfield cell viability model for screening matrix-embedded organoids	9
Luminescence Energy Transfer–Based Screening and Target Engagement Approaches for Chemical Biology and Drug Discovery	9
Identification of Small-Molecule Inhibitors of Neutral Ceramidase (nCDase) via Target-Based High-Throughput Screening	9
Development of a Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay for the Inhibition of Keap1–Nrf2 Protein–Protein Interaction	9
A Perspective on Synthetic Biology in Drug Discovery and Development—Current Impact and Future Opportunities	9
Epithelial Barrier Integrity Profiling: Combined Approach Using Cellular Junctional Complex Imaging and Transepithelial Electrical Resistance	9
A Comparative Study of Target Engagement Assays for HDAC1 Inhibitor Profiling	9
Development of a High-Throughput Screening Assay to Identify Inhibitors of the Major M17-Leucyl Aminopeptidase from Trypanosoma cruzi Using RapidFire Mass Spectrometry	9
Characterizations of the Urate Transporter, GLUT9, and Its Potent Inhibitors by Patch-Clamp Technique	8
The Extensive and Expensive Impacts of HEp-2 [HeLa], Intestine 407 [HeLa], and Other False Cell Lines in Journal Publications	8
Fragment-based screening: A new paradigm for ligand and target discovery	8
Based on Principles and Insights of COVID-19 Epidemiology, Genome Sequencing, and Pathogenesis: Retrospective Analysis of Sinigrin and ProlixinRX (Fluphenazine) Provides Off-Label Drug Candidates	8
A High-Throughput Image Cytometry Method for the Formation, Morphometric, and Viability Analysis of Drug-Treated Mammospheres	8
Operationalizing the Use of Biofabricated Tissue Models as Preclinical Screening Platforms for Drug Discovery and Development	8
High-Throughput Image-Based Aggresome Quantification	8
Development of a Novel Label-Free and High-Throughput Arginase-1 Assay Using Self-Assembled Monolayer Desorption Ionization Mass Spectrometry	8
A multiparametric calcium signal screening platform using iPSC-derived cortical neural spheroids.	8
Point-of-use, automated fabrication of a 3D human liver model supplemented with human adipose microvessels	8
Automation of Organoid Cultures: Current Protocols and Applications	8
High-Throughput Screening Assays for Cancer Immunotherapy Targets: Ectonucleotidases CD39 and CD73	7
Hit Discovery for Public Target Programs in the European Lead Factory: Experiences and Output from Assay Development and Ultra-High-Throughput Screening	7
High-Throughput Affinity Selection Mass Spectrometry Using SAMDI-MS to Identify Small-Molecule Binders of the Human Rhinovirus 3C Protease	7
Treating Cells as Reagents to Design Reproducible Assays	7
Regenerable Biosensors for Small-Molecule Kinetic Characterization Using SPR	7
Multifunctional profiling of triple-negative breast cancer patient-derived tumoroids for disease modeling	7
Development of a Testing Funnel for Identification of Small-Molecule Modulators Targeting Secretin Receptors	7
Mass spectrometry-based proteomics of 3D cell culture: A useful tool to validate culture of spheroids and organoids	7
Correlation of Optical and Automated Patch Clamp Electrophysiology for Identification of NaV1.7 Inhibitors	7
Saporin, a Polynucleotide–Adenosine Nucleosidase, May Be an Efficacious Therapeutic Agent for SARS-CoV-2 Infection	7
Delivering Robust Candidates to the Drug Pipeline through Computational Analysis of Arrayed CRISPR Screens	6
High-throughput cell-based assays for identifying antagonists of multiple smoking-associated human nicotinic acetylcholine receptor subtypes	6
Screening for modulators of autism spectrum disorder using induced human neurons	6
High-Throughput Fluorescence-Based Activity Assay for Arginase-1	6
The Use of Informer Sets in Screening: Perspectives on an Efficient Strategy to Identify New Probes	6
A Perspective on Expanding Our Understanding of Cancer Treatments by Integrating Approaches from the Biological and Physical Sciences	6
Maintaining a High-Quality Screening Collection: The GSK Experience	6
High-throughput approaches to uncover synergistic drug combinations in leukemia	6
Developing an Arrayed CRISPR-Cas9 Co-Culture Screen for Immuno-Oncology Target ID	6
A perspective on the discovery of enzyme activators	6
Automating Complex, Multistep Processes on a Single Robotic Platform to Generate Reproducible Phosphoproteomic Data	6
Development of a High-Throughput, Compound-Multiplexed Fluorescence Polarization Assay to Identify ATG5–ATG16L1 Protein–Protein Interaction Inhibitors	6
Addressing Compound Reactivity and Aggregation Assay Interferences: Case Studies of Biochemical High-Throughput Screening Campaigns Benefiting from the National Institutes of Health Assay Guidance Man	6
A Novel Luminescence-Based High-Throughput Approach for Cellular Resolution of Protein Ubiquitination Using Tandem Ubiquitin Binding Entities (TUBEs)	6
Assay Guidance Manual for Drug Discovery: Robust or Go Bust	6
Development of a High-Throughput Screening-Compatible Assay for Discovery of GPR3 Inverse Agonists Using a cAMP Biosensor	6
Applications of Functional Genomics for Drug Discovery	6
Identification of Compounds That Promote Readthrough of Premature Termination Codons in the CFTR	6
Deep Learning-Based HCS Image Analysis for the Enterprise	6
Development of a high-throughput TR-FRET screening assay for LAG-3/FGL1 interaction	6
A Whole Genome-Wide Arrayed CRISPR Screen in Primary Organ Fibroblasts to Identify Regulators of Kidney Fibrosis	6
Epithelial 3D-spheroids as a tool to study air pollutant-induced lung pathology	5
Functional Genomics for Target Identification	5
In Silico Selection of Gp120 ssDNA Aptamer to HIV-1	5
Potential Repurposed Therapeutics and New Vaccines against COVID-19 and Their Clinical Status	5
In Vitro Ubiquitination Platform Identifies Methyl Ellipticiniums as Ubiquitin Ligase Inhibitors	5
A Solid Supported Membrane-Based Technology for Electrophysical Screening of B0AT1-Modulating Compounds	5
A “Target Class” Screen to Identify Activators of Two-Pore Domain Potassium (K2P) Channels	5
A high-throughput MALDI-TOF MS biochemical screen for small molecule inhibitors of the antigen aminopeptidase ERAP1	5
The CellRaft AIRⓇ system: A novel system enabling organoid imaging, identification, and isolation	5
High-Throughput Screening and Triage Assays Identify Small Molecules Targeting c-MYC in Cancer Cells	5
Method Development and Application of an Accelerated Solution Stability Screen for Drug Discovery	5
Complex Tumor Spheroids, a Tissue-Mimicking Tumor Model, for Drug Discovery and Precision Medicine	5
High throughput screening of 0.5 million compounds against CRAF using Alpha CETSAⓇ	5
Development of a Microscale Thermophoresis-Based Method for Screening and Characterizing Inhibitors of the Methyl-Lysine Reader Protein MRG15	5
Replenishing the malaria drug discovery pipeline: Screening and hit evaluation of the MMV Hit Generation Library 1 (HGL1) against asexual blood stage Plasmodium falciparum, using a nano luciferase rep	5
Development of high-throughput lacrimal gland organoid platforms for drug discovery in dry eye disease	5
A New Method for Screening Natural Products to Stimulate IFN-γ Production in Jurkat Human T Lymphocytes	5
Two Forms of Tyrosyl-tRNA Synthetase from Pseudomonas aeruginosa: Characterization and Discovery of Inhibitory Compounds	5
Development of a High-Throughput Assay to Identify Inhibitors of ENPP1	4
A Novel Screening Approach for the Dissection of Cellular Regulatory Networks of NF-κB Using Arrayed CRISPR gRNA Libraries	4
Discovery of hit compounds for methyl-lysine reader proteins from a target class DNA-encoded library	4
HTS driven by fluorescence lifetime detection of FRET identifies activators and inhibitors of cardiac myosin	4
Image-Based Marker-Free Screening of GABAA Agonists, Antagonists, and Modulators	4

NMR Reporter Assays for the Quantification of Weak-Affinity Receptor–Ligand Interactions	4
Single-Cell Distribution Analysis of AR Levels by High-Throughput Microscopy in Cell Models: Application for Testing Endocrine-Disrupting Chemicals	4
In-Plate Cryopreservation of 2D and 3D Cell Models: Innovative Tools for Biomedical Research and Preclinical Drug Discovery	4
A Mechanistic High-Content Analysis Assay Using a Chimeric Androgen Receptor That Rapidly Characterizes Androgenic Chemicals	4
A Novel High-Throughput FLIPR Tetra–Based Method for Capturing Highly Confluent Kinetic Data for Structure–Kinetic Relationship Guided Early Drug Discovery	4
A novel high-throughput screening strategy for targeting alpha-synuclein and other long-lived proteins	4
High-Throughput Screening to Identify Small Molecules That Selectively Inhibit APOL1 Protein Level in Podocytes	4
A High-Throughput Cellular Screening Assay for Small-Molecule Inhibitors and Activators of Cytoplasmic Dynein-1-Based Cargo Transport	4
Screening for positive allosteric modulators of cholecystokinin type 1 receptor potentially useful for management of obesity	4
Identification of positive modulators of TRPM5 channel from a high-throughput screen using a fluorescent membrane potential assay	4
Application of a High-Content Screening Assay Utilizing Primary Human Lung Fibroblasts to Identify Antifibrotic Drugs for Rapid Repurposing in COVID-19 Patients	3
Automation of high-throughput mRNA-seq library preparation: a robust, hands-free and time efficient methodology	3
Validation of a High-Throughput Calcium Mobilization Assay for the Human Trace Amine-Associated Receptor 1	3
The New Frontier of Functional Genomics: From Chromatin Architecture and Noncoding RNAs to Therapeutic Targets	3
Rapid Compound Integrity Assessment for High-Throughput Screening Hit Triaging	3
Utilising acoustic mist ionisation mass spectrometry to identify redox cycling compounds in high throughput screening outputs	3
Fast Mek1 Hit Identification with TRIC Technology Correlates Well with Other Biophysical Methods	3
In Vitro Pharmacokinetic/Pharmacodynamic Modeling of HIV Latency Reversal by Novel HDAC Inhibitors Using an Automated Platform	3
Evolution and impact of high content imaging	3
Robustness of NanoBiT luciferase complementation technology in the presence of widely used kinase inhibitors	3
High-content phenotypic screen to identify small molecule enhancers of Parkin-dependent ubiquitination and mitophagy	3
Unbiased High-Throughput Drug Combination Pilot Screening Identifies Synergistic Drug Combinations Effective against Patient-Derived and Drug-Resistant Melanoma Cell Lines	3
Identification and Kinetic Characterization of Serum- and Glucocorticoid-Regulated Kinase Inhibitors Using a Fluorescence Polarization–Based Assay	3
Protocol for 3D drug sensitivity and resistance testing of patient-derived cancer cells in 384-well plates	3
Keeping It Clean: The Cell Culture Quality Control Experience at the National Center for Advancing Translational Sciences	3
Generation of a Monoclonal Antibody against D-Dimer Using HTS-Based LiCA	3
Label-free high-throughput screening via acoustic ejection mass spectrometry put into practice	3
Differential analyte derivatization enables unbiased MALDI-TOF-based high-throughput screening: A proof-of-concept study for the discovery of catechol-o-methyltransferase inhibitors	3
Functional and Pharmacological Comparison of Human and Mouse Na+/Taurocholate Cotransporting Polypeptide (NTCP)	3
Optimization of a High-Throughput Cell-Based Screening Strategy to Identify Small-Molecule Inhibitors of IL-23 Signaling	3
Deep Learning Image Analysis of High-Throughput Toxicology Assay Images	3
DeepTI: A deep learning-based framework decoding tumor-immune interactions for precision immunotherapy in oncology	3
Automated high-content imaging in iPSC-derived neuronal progenitors	3
High throughput screening for compounds to the orphan nuclear receptor NR2F6	3
Leveraging Automation toward Development of a High-Throughput Gene Expression Profiling Platform	3
P-Glycoprotein-Mediated Efflux Using a Rapidly Maturing Caco2 Clone (CLEFF4) in Only 5 Days without Requiring Modified Growth Medium	3
High-Throughput Phenotypic Assay for Compounds That Influence Mitochondrial Health Using iPSC-Derived Human Neurons	3
Quantitative Automated Assays in Living Cells to Screen for Inhibitors of Hemichannel Function	3
Adipocyte-based high throughput screening for anti-obesity drug discovery: Current status and future perspectives	3
Discovery of Novel HCN4 Blockers with Unique Blocking Kinetics and Binding Properties	3
Phenotypic Screening Following Transcriptomic Deconvolution to Identify Transcription Factors Mediating Axon Growth Induced by a Kinase Inhibitor	3
Development and Optimization of a High-Content Analysis Platform to Identify Suppressors of Lamin B1 Overexpression as a Therapeutic Strategy for Autosomal Dominant Leukodystrophy	3
High throughput screening for drugs that inhibit 3C-like protease in SARS-CoV-2	3
High-Throughput Mechanism of Inhibition	3
Identification of Two Non-Peptidergic Small Molecule Inhibitors of CBX2 Binding to K27 Trimethylated Oligonucleosomes	3
Therapeutic and Vaccine Options for COVID-19: Status after Six Months of the Disease Outbreak	3
Development of a High-Throughput Affinity Mass Spectrometry (AMS) Platform Using Laser Diode Thermal Desorption Ionization Coupled to Mass Spectrometry (LDTD-MS)	3