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Assay Guidance Manual for Drug Discovery: Robust or Go Bust
Assay Guidance Manual for Drug Discovery: Robust or Go Bust
1. Freedman, L. P., Cockburn, I. M., Simcoe, T. S. The Economics of Reproducibility in Preclinical Research. PLoS Biol. 20...
Complex Tumor Spheroids, a Tissue-Mimicking Tumor Model, for Drug Discovery and Precision Medicine
Complex Tumor Spheroids, a Tissue-Mimicking Tumor Model, for Drug Discovery and Precision Medicine
Malignant tumors are complex tissues composed of malignant cells, vascular cells, structural mesenchymal cells including p...
The Extensive and Expensive Impacts of HEp-2 [HeLa], Intestine 407 [HeLa], and Other False Cell Lines in Journal Publications
The Extensive and Expensive Impacts of HEp-2 [HeLa], Intestine 407 [HeLa], and Other False Cell Lines in Journal Publications
Cell lines are essential models for biomedical research. However, they have a common and important problem that needs to b...
Advances in High-Content Imaging and Informatics: A Joint Special Collection with Society for Biomolecular Imaging and Informatics and SLAS
Advances in High-Content Imaging and Informatics: A Joint Special Collection with Society for Biomolecular Imaging and Informatics and SLAS
Access to society journal content varies across our titles. If you have access to a journal via a society or association ...
Flexible Fitting of PROTAC Concentration–Response Curves with Changepoint Gaussian Processes
Flexible Fitting of PROTAC Concentration–Response Curves with Changepoint Gaussian Processes
A proteolysis-targeting chimera (PROTAC) is a new technology that marks proteins for degradation in a highly specific mann...
Treating Cells as Reagents to Design Reproducible Assays
Treating Cells as Reagents to Design Reproducible Assays
The reproducibility of high-throughput cell-based assays is dependent on having a consistent source of cells for each expe...
Addressing Unusual Assay Variability with Robust Statistics
Addressing Unusual Assay Variability with Robust Statistics
Well-behaved, in vitro bioassays generally produce normally distributed values in their primary (efficacy) data. According...
Applications of Biophysics in Early Drug Discovery
Applications of Biophysics in Early Drug Discovery
1. Genick, C. C., Barlier, D., Monna, D. Applications of Biophysics in High-Throughput Screening Hit Validation. J. Biomol...
Luminescence Energy Transfer–Based Screening and Target Engagement Approaches for Chemical Biology and Drug Discovery
Luminescence Energy Transfer–Based Screening and Target Engagement Approaches for Chemical Biology and Drug Discovery
Luminescence is characterized by the spontaneous emission of light resulting from either chemical or biological reactions....
Acoustic Ejection Mass Spectrometry: A Fully Automatable Technology for High-Throughput Screening in Drug Discovery
Acoustic Ejection Mass Spectrometry: A Fully Automatable Technology for High-Throughput Screening in Drug Discovery
Acoustic droplet ejection (ADE)–open port interface (OPI)–mass spectrometry (MS) has recently been introduced as a versati...
Approaches for Prioritizing High-Quality Chemical Matter in Chemical Probe and Drug Discovery
Approaches for Prioritizing High-Quality Chemical Matter in Chemical Probe and Drug Discovery
Access to society journal content varies across our titles. If you have access to a journal via a society or association ...
Operationalizing the Use of Biofabricated Tissue Models as Preclinical Screening Platforms for Drug Discovery and Development
Operationalizing the Use of Biofabricated Tissue Models as Preclinical Screening Platforms for Drug Discovery and Development
A wide range of complex in vitro models (CIVMs) are being developed for scientific research and preclinical drug efficacy ...
Development of an Image-Based HCS-Compatible Method for Endothelial Barrier Function Assessment
Development of an Image-Based HCS-Compatible Method for Endothelial Barrier Function Assessment
The recent renascence of phenotypic drug discovery (PDD) is catalyzed by its ability to identify first-in-class drugs and ...
Identification of Compounds for Butyrylcholinesterase Inhibition
Identification of Compounds for Butyrylcholinesterase Inhibition
Butyrylcholinesterase (BChE) is a nonspecific cholinesterase enzyme that hydrolyzes choline-based esters. BChE plays a cri...
ASCT1 and ASCT2: Brother and Sister?
ASCT1 and ASCT2: Brother and Sister?
The SLC1 family includes seven members divided into two groups, namely, EAATs and ASCTs, that share similar 3D architectur...
Fast Mek1 Hit Identification with TRIC Technology Correlates Well with Other Biophysical Methods
Fast Mek1 Hit Identification with TRIC Technology Correlates Well with Other Biophysical Methods
The variety and complexity of drug targets are expanding rapidly. At the same time, there is significant interest in explo...
The Impact of Assay Design on Medicinal Chemistry: Case Studies
The Impact of Assay Design on Medicinal Chemistry: Case Studies
A diverse range of biochemical and cellular assays are used by medicinal chemists to guide compound optimization. The data...
Addressing Compound Reactivity and Aggregation Assay Interferences: Case Studies of Biochemical High-Throughput Screening Campaigns Benefiting from the National Institutes of Health Assay Guidance Manual Guidelines
Addressing Compound Reactivity and Aggregation Assay Interferences: Case Studies of Biochemical High-Throughput Screening Campaigns Benefiting from the National Institutes of Health Assay Guidance Manual Guidelines
Compound-dependent assay interferences represent a continued burden in drug and chemical probe discovery. The open-source ...
High-Throughput Screening to Identify Small Molecules That Selectively Inhibit APOL1 Protein Level in Podocytes
High-Throughput Screening to Identify Small Molecules That Selectively Inhibit APOL1 Protein Level in Podocytes
High-throughput phenotypic screening is a key driver for the identification of novel chemical matter in drug discovery for...
Phenotypic Screening Following Transcriptomic Deconvolution to Identify Transcription Factors Mediating Axon Growth Induced by a Kinase Inhibitor
Phenotypic Screening Following Transcriptomic Deconvolution to Identify Transcription Factors Mediating Axon Growth Induced by a Kinase Inhibitor
After injury to the central nervous system (CNS), both neuron-intrinsic limitations on regenerative responses and inhibito...
The Drug Factory: Industrializing How New Drugs Are Found
The Drug Factory: Industrializing How New Drugs Are Found
In this perspective, the authors paint a vision for industrializing drug discovery with an “atoms and bits” approach. This...
Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors
Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors
The COVID-19 pandemic has clearly brought the healthcare systems worldwide to a breaking point, along with devastating soc...
Validating ADME QSAR Models Using Marketed Drugs
Validating ADME QSAR Models Using Marketed Drugs
Problems with drug ADME are responsible for many clinical failures. By understanding the ADME properties of marketed drugs...
Automation of Organoid Cultures: Current Protocols and Applications
Automation of Organoid Cultures: Current Protocols and Applications
Organoids are three-dimensional, functional structures that mimic in vivo organs. They offer new opportunities for the mod...
A High-Content Screening Assay for Small Molecules That Stabilize Mutant Triose Phosphate Isomerase (TPI) as Treatments for TPI Deficiency
A High-Content Screening Assay for Small Molecules That Stabilize Mutant Triose Phosphate Isomerase (TPI) as Treatments for TPI Deficiency
Triose phosphate isomerase deficiency (TPI Df) is an untreatable, childhood-onset glycolytic enzymopathy. Patients typical...
Evaluating Very Deep Convolutional Neural Networks for Nucleus Segmentation from Brightfield Cell Microscopy Images
Evaluating Very Deep Convolutional Neural Networks for Nucleus Segmentation from Brightfield Cell Microscopy Images
Advances in microscopy have increased output data volumes, and powerful image analysis methods are required to match. In p...
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening
SMYD3 (SET and MYND domain-containing protein 3) is a protein lysine methyltransferase that was initially described as an ...
A Phenotypic Approach for the Identification of New Molecules for Targeted Protein Degradation Applications
A Phenotypic Approach for the Identification of New Molecules for Targeted Protein Degradation Applications
Targeted protein degradation is an emerging new strategy for the modulation of intracellular protein levels with applicati...
Discovery of Novel HCN4 Blockers with Unique Blocking Kinetics and Binding Properties
Discovery of Novel HCN4 Blockers with Unique Blocking Kinetics and Binding Properties
The hyperpolarization-activated cyclic nucleotide-gated 4 (HCN4) channel underlies the pacemaker currents, called “If,” in...
waveRAPID—A Robust Assay for High-Throughput Kinetic Screens with the Creoptix WAVEsystem
waveRAPID—A Robust Assay for High-Throughput Kinetic Screens with the Creoptix WAVEsystem
Surface-based biophysical methods for measuring binding kinetics of molecular interactions, such as surface plasmon resona...
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