BellBrook Labs
1232 Fourier Drive, Suite 115
Madison, Wisconsin 53717 USA
(608) 443-2400
info@bellbrooklabs.com
Targeting Sirtuins in Epigenetic Regulation: A High-Throughput Assay for Drug Discovery
In this webinar, you will learn:
- Why SIRT enzymes are emerging as key targets in epigenetics and oncology
- How our assay overcomes limitations of traditional methods by measuring real time enzyme activity.
- Optimization strategies for NAD, substrate, and enzyme concentrations under initial velocity conditions
- Validation of the assay using SIRT1 and SIRT2 with robust performance (Z’ > 0.7) and strong agreement between FP and TR-FRET readouts
- Results from screening a 1,280-compound bioactive library and follow-up dose-response characterization of hits
- How this platform supports HTS, structure-activity relationship (SAR), and lead discovery for SIRT inhibitor programs
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Measuring Helicase Activity With Transcreener and Heliscreener
In this webinar, you will learn:
- The biological roles and mechanistic diversity of DEAD-box helicases in RNA metabolism and innate immune signaling.
- How to apply biochemical HTS assays to measure helicase ATPase and unwinding activity with precision and reproducibility.
- How the Transcreener® ADP² Assay and Heliscreener™ Unwinding Assay complement each other for detecting helicase function and inhibitor profiling.
- Practical examples of screening and dose–response validation using DDX3, DDX5, DHX9, and DDX17.
- Key considerations for selecting and optimizing assay formats for small-molecule drug discovery targeting helicases.
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Targeting VPS4A and VPS4B Synthetic Lethality A New Tool for ATPase Drug Discovery
In this webinar, you will learn:
- Why VPS4A and VPS4B are compelling oncology targets – and how their synthetic lethality opens new therapeutic avenues
- How our HTS-compatible assay was developed using purified enzymes and optimized for initial velocity detection
- How we validated the assay with Z’ greater than 0.7 and identified two potent hits—BVT948 and polygodial—from a known bioactives library
- Strategies for minimizing off-target effects when working with ATPase inhibitors
- How this assay platform supports HTS, SAR, and hit-to-lead development for drug discovery teams
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Targeting PARP Synthetic Lethality An HTS Assay for Cancer Drug Discovery
In this webinar, you will learn:
- Why PARP inhibition is a cornerstone of synthetic lethality in oncology
- How our HTS-compatible assay was optimized to minimize compound interference and ensure robust pADPr detection
- How we validated the assay with Z’ greater than 0.8 using PARP1 and PARP2 under initial velocity conditions
- Results from screening over 4,000 compounds, including successful identification of known inhibitors (Olaparib, Veliparib, Rucaparib, PJ34) with published IC₅₀ alignment
- How this assay platform supports HTS, SAR, and lead discovery for PARP inhibitor programs
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Development of HTS Enzymatic Assays for RNA Helicases: DDX3, DDX5, DDX17, RIG-I, and MDA5
In this webinar, you will learn:
- Developing HTS assays for DDX3, DDX17, and DDX5, which have all been implicated in cancer, and the Rig-I-like receptor (RLR) helicases, RIG-I and MDA5, which trigger expression of type I interferons important for tumor immunity
- Determining RNA substrate and cofactor requirements and kinetic parameters with the purified enzymes and optimizing the assays for initial velocity detection of RNA-dependent ATPase activity with a Z’ value greater than 0.7
- Validating each of the helicase ATPase assays for HTS by screening a collection of bioactives (Tocris 2.0) and confirming the hits in dose-response mode with the enzymatic assays and with thermal shift assays to confirm target binding
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Using the Transcreener ADPR Assay for Drug Discovery Targeting DNA Damage Repair & Innate Immunity
In this webinar, you will learn:
- How the Transcreener ADPR Assay will provide a reliable and robust tool for the discovery of CD38 and PARG inhibitors
- The sensitivity and selectivity of the ADPR Assay, and its ability to obtain robust assay signals (Greater than 100 mP) for initial velocity detection with picomolar concentrations of CD38 and PARG and Z’ values greater than 0.8
- Validation studies that include a pilot screen of 1280 pharmacologically active molecules and does response assays to measure the IC50 of confirmed hits
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Interrogating GTPase Effector Proteins Screening GAPs and GEFs with the Transcreener GDP Assay
In this webinar, you will learn:
- How the Transcreener® GDP Assay enables robust screening and profiling of GTPases using direct immunodetection of GDP with fluorescence polarization (FP), fluorescence intensity (FI) or TR-FRET readouts.
- How to measure GTPase-GEF catalytic activity based on stimulation of steady state GDP formation, using the Transcreener® GDP Assay. Examples of two DOCK family Rho GEFs, Dbl and P-Rex1 with their respective Rho GTPase substrates, RhoA, CDC42 and P-Rex1 will be used as case studies.
- Development of a robust HTS method for identifying inhibitors of members of the “regulator of G-protein signaling” (RGS)-protein superfamily that act as GAPs for heterotrimeric G-protein alpha subunits, using Transcreener® GDP assay.
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Targeting Kinases Involved in the Innate Immune Response
Clinical trials continue to determine whether therapeutic modulation of kinases can be used to suppress the immune system in autoimmune diseases or stimulate for antiviral and cancer immunotherapy. The discovery and characterization of small molecule modulators have aided these efforts. The Transcreener ADP² Kinase Assay meets this need as it relies on direct ADP detection to measure the activity of virtually any kinase. The method has been extensively validated for kinase discovery programs since 2007. This webinar provides five examples of how Transcreener allowed rapid assay development to enable screening and dose-response measurements. The innate immunity-associated kinases targeted in this webinar include: AMP-Activated Kinase (AMPK) Janus Kinase 1 and 3 (JAK1 and JAK3) TANK-Binding Kinase 1 (TBK1) Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) IκB Kinase (IKK-β).
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Streamline cGAS Inhibitor Discovery with the Transcreener® cGAS Assay
In this webinar, we will discuss:
- Sensitive detection of cGAS initial velocity in the presence of saturating ATP and GTP concentrations
- Providing overnight and reagent signal stability that provide flexibility in liquid handling
- Measuring accurate IC50 values
- Determining the inhibitor mechanism of action
- Using cGAS assays for kinetic studies such as residence-time determination
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Transcreener CD73 Assay Leveraging Nucleotide Detection to Measure Adenosine
This talk focused on the use of Transcreener® ADO assay to measure adenosine, both in basic research and drug discovery.
Topics covered include:
- Developing a coupled assay for measuring CD73 enzyme activity
- Establishing high-throughput screening conditions
- Setting up a screen
- Running dose-response curves with a focus on data analysis
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Analyzing Kinase Inhibitor Residence Times using the Transcreener ADP Assay
Topics covered include:
- How the Transcreener® HTS platform enables direct, homogenous detection of ADP and other nucleotides.
- An overview of drug residence times as a lead development parameter.
- How to employ the jump dilution method to measure kinase inhibitor dissociation rates using the Transcreener® ADP assay.
- Data analysis considerations and methods.
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Streamline HTS and Lead Discovery with the Transcreener ADP Kinase Assay
Topics covered include:
- Sensitive detection of kinase initial velocity over a broad range of ATP concentrations, critical for screening such a diverse class of targets
- Compound interference comparisons between Transcreener and other HTS assays
- Compatibility with 1536 well-miniaturized formats along with overnight and reagent signal stability that provide flexibility in liquid handling
- Using kinase assays for kinetic studies such as residence time determination
- Measuring accurate IC50 values, even for potent kinase inhibitors due to robust assay signal at low enzyme concentration
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The AptaFluor™ SAH Assay: A Homogeneous, Universal HTS Ready Methyltransferase Assay
In this webinar we will discuss:
- Engineering a microbial riboswitch for direct detection of SAH in a homogeneous format with a positive TR-FRET readout
- Demonstrated assay robustness for use in hit identification and characterization studies including reagent stability, signal stability, and sensitivity
- Comparison of other assay methods with the new AptaFluor SAH Methyltransferase Assay
- Unparalleled assay sensitivity that can be harnessed for use with low turnover methyltransferase enzymes and SAM concentrations as low as 100 nM
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Development of Ectonucleotidase Assay Methods Using the Transcreener® HTS Assay Platform
In this webinar we will discuss:
- Assay development for CD39 using the Transcreener® AMP/GMP Assay with fluorescence polarization and TR-FRET readouts
- Demonstrated assay robustness for use in high-throughput screening
- Inhibitor potency profiling for CD39
- Recent external publications using Transcreener® HTS assays for studying ectonucleotidase activity
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