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Determination of Drug Residence Time in an HTS Format using Kinetic Analysis with the Transcreener® ADP2 Assay

BellBrook Labs
19 Jun 2016

This poster describes a systematic approach to determine the residence time of compounds using Abl1 and Aurora C as targets and several well characterized ATP-competitive drugs. Residence time can be determined by equilibrium binding measurements using methods such as surface plasmon resonance (SPR), which provides highly quantitative data but requires costly instrumentation and long experimental timelines. Transcreener® ADP2 Assays offer a highly sensitive and versatile method for estimating drug residence times for kinases using a multimode fluorescent plate reader.

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Transcreener® ADP² Kinase Assays

BellBrook Labs

The Transcreener® ADP² Kinase Assay Kit universally detects ADP produced by any kinase or ATPase using a direct mix‑and‑read format, eliminating coupling steps. Available in FP, FI, and TR‑FRET formats with far‑red tracers to minimize interference, it's HTS-ready across 96‑, 384‑, and 1536‑well plates with robust Z' ≥ 0.7 performance.

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Microplate Readers / DetectorsMicroplate readers are used to automate the detection and analysis of labeled or label-free components in microplates during assays or live-cell monitoring. Microplate readers are generally distinguished by their mode of detection. Types include absorbance, luminescence, fluorescence intensity, fluorescence polarization, TRF / FRET and multimode microplate readers. Microplate readers deliver a high throughput of samples by reading multiple wells simultaneously, with the 96-well format the most commonly used. As a result, microplate readers are often used in the drug discovery, bioassays, research and pharmaceutical industries for screening applications. Microplate loading can also be automated, with robotic microplate stackers to increase throughput. Find the best microplate readers in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Assay AssemblyAssay Assembly is technique used in drug discovery to develop assays to test the cytotoxicity, genotoxicity, or other activities of a compound on a cell. Assay assembly requires chip assembly, a delivery system and a detection and analysis method. Beneficial features of assay kits or automated systems include high-throughput, high speed and sensitivity and low signal to noise ratio.Bioprocessing / FermentationBioprocessing is the use of biological materials to perform commercial, scientific or medical research processes. Biological materials used include cells, enzymes and organisms. Usually bioprocessing requires a batch or continuous bioreactor such as a fermentor or cell culture system. The advantages of using a reactor include high productivity, easy configuration, adjustable values and automation.Assay DevelopmentThe process of proving an assay to be sensitive with respect to the target is known as assay development. The assay should be able to characterize novel compounds and measure the potency of these compounds against a validated biological target.Compound ScreeningCompound screening is a method used to discover specific compounds that could be promising candidates for pharmaceutical use. This potential is identified when compounds interact with the target protein during screening and could therefore be carried forward in the drug development process.ATP MonitoringSurface Plasmon ResonanceQuantitative AnalysesQuantitative analyses involve measuring the amount or concentration of a substance in a sample using analytical techniques. These analyses are essential in fields like chemistry, biology, and environmental science. Explore quantitative analysis tools in our peer-reviewed product directory; compare products, check reviews, and get pricing directly from manufacturers.Fluorescence Based AssayFluorescence based assays are widely used in life science research and high-throughput screening to measure a broad range of cellular activities.

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Determination of Drug Residence Time in an HTS Format using Kinetic Analysis with the Transcreener® ADP2 Assay