Measuring Kinase Inhibitor Residence Times with the Transcreener® ADP2 FP Assay
This Application Note provides a protocol, experimental examples, and data analysis guidelines for using the Transcreener® ADP2 FP Assay to determine dissociation rates and residence times for kinase inhibitors using simple HTS-compatible methods.
Measuring Phosphodiesterase Inhibitor Residence Times with the Transcreener® AMP2/GMP2 FP Assay
This Case Study uses a jump-dilution method with the Transcreener® AMP2/GMP2 FP Assay to determine the residence times for PDE inhibitors.
Discovery of GALNT3 Inhibitors Using a Universal Glycosyltransferase Assay and Orthogonal Pooled Screening
This Case Study shows how to develop an HTS workflow for glycosyltransferases (GTs) with an optimized Transcreener® UDP2 Assay (FP and TR-FRET formats), use the assay to measure GT activity and determine Km values, run a pilot screen for specific enzyme inhibitors on 8,000 compounds using Orthogonal Pooled Screening (OPS™) technology, and confirm, validate, and characterize hits.
Exploring the Sumoylation Cascade using the Transcreener® AMP2/GMP2 Assay
This Case Study helps you learn how to detect AMP formed by E1 alone or the complete SUMO ligase cascade in a homogenous, mix and read assay and determine the potency of SUMO ligase inhibitors.
Selective Detection of LRRK2 GTPase Activity with the Transcreener® GDP Assay
This Case Study helps you learn how BellBrook Labs developed a selective and sensitive, HTS-ready assay for the GTPase domain of LRRK2 using the Transcreener® GDP FP Assay.
Customer Success Story:
Development of a High-Throughput Screening Assay to Identify Inhibitors of the de novo Purine Biosynthetic Pathway
David Whalley et al.
This Case Study helps you learn more about David Whalley and his success using the BellBrook Labs Transcreener® ADP assay. David leveraged the Transcreener® ADP assay to identify inhibitors of PAICS, a key enzyme in the de novo purine biosynthesis pathway that has been suggested as an attractive drug target for cancer.
Orthogonal Pooled Screening: HTS with 5X higher efficiency, using 5X fewer resources
In this Tutorial, explore what orthogonal pooled screening (OPS™) is, how the OPS™ Platform works, why you should consider using the OPS™ Platform and the LCGC library, and what benefits the OPS™ Platform provides in terms of efficiency, resources, and results.
Homogenous Transcreener® UDP2 TR-FRET Assay for High Throughput Screening with Glycosyltransferases
In this Tutorial, learn how to use Transcreener® HTS assays for direct detection of glycosyltransferases that use different sugar-nucleotide donors, how to measure enzyme activity and inhibitor dose responses for several GTs, including human fucosyltransferase, glucosylceramide synthase, galactose N-acetyltransferases, β1-4 galactosyltransferase, sialyltransferase and C. dificile Toxin B.
Transcreener® Assay Development Services
In this Tutorial, learn about our Assay Development Services, including our quick enzyme activity test, options for assay optimization and inhibitor profiling, and pilot screen capabilities.
Profiling Phosphodiesterases with the Transcreener® AMP2/GMP2 TR-FRET Assay
In this Tutorial, learn about our Transcreener® AMP2/GMP2 TR-FRET Assay, with a highly specific antibody and a simple, mix-and-read format, lighting the way in cyclic nucleotide phosphodiesterase profiling.
Transcreener® ADP2 Assays for universal screening and profiling of any kinase or ATPase
In this Tutorial, learn about our Transcreener® ADP2 Assays and their single addition, mix-and-read assay format compatible with automated high throughput screening and profiling protocols, the reliable Transcreener® assay reagents and assay signals that simplify your workflows, how enzyme costs are reduced and fewer false positives are observed.
Probing p97 ATPase with the Transcreener® ADP2 ATPase Assay
In this case study, BellBrooks’ scientific team optimized enzyme reaction and detection conditions that produced outstanding assay windows and Z’ values for both forms of the enzyme within one week.
Streamlining Kinase Screening and Profiling with Transcreener® ADP2 Assays
In this Tutorial, learn about our Transcreener® ADP2 Assays, our instrument validation program to insure optimal performance on all major multimode readers, calibration line for ATP concentrations from 0.1 to 1,000 μM, use of EC40–EC80 enzyme concentration, and the ability to determine accurate inhibitor IC50 values directly from raw fluorescence data, eliminating the need for standard curves.
Transcreener® HTS Assays for Epigenetic Enzymes
In this Tutorial, learn how each of these four Transcreener® assays enables detection of epigenetic enzymes in a robust, HTS-ready format: ADP2 Assay for kinases, AMP2/GMP2 Assay for Ub and Sumo ligases, EPIGEN Methyltransferase Assay for HMTs, and EPIGEN Acetyltransferase Assay for HATs.
Validation of Reaction Biology’s recombinant human methyltransferases in the Transcreener® Epigen Methylatransferase Assay
In this Tutorial, you can learn how BellBrook’s Transcreener® EPIGEN MT Assay provides universal detection of histone and DNA methyltransferases with the sensitivity and robustness needed for industrial HTS as well as how we are determining the optimal reaction conditions to produce an outstanding assay window under initial velocity conditions for each of RBCs enzymes, including challenging targets such as NSD2, MLL4 and EzH2.
Screening for inhibitors of RGS protein GAP activity using the RGScreen Assay
In this Tutorial, you can learn how BellBrook overcame the technical barriers to enable screening for RGS inhibitors in a direct biochemical HTS assay format, why RGS proteins are emerging as an exciting new class of drug targets, how RGS GAP activity can be easily measured in a homogeneous fluorescent assay format, and how 7 RGS4-specific inhibitors were identified from a 960 compound pilot screen.