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BellBrook Labs Publishes “A Guide to Measuring Drug-Target Residence Times with Biochemical Assays”
Date:8/31/2018

In recent years researchers have been increasing efforts to measure inhibitor residence times as a component of drug discovery programs. Longer-target engagement can result in improved efficacy and reduced side effects. Other methods of deriving these residence times are low throughput, require expensive instrumentation, or require the alteration of the molecules involved. The limitations of these methods make it challenging to prioritize compounds within the time constraints of a drug discovery program. The ability to effectively measure drug-target residence time in a high throughput format gives scientists the tools to effectively prioritize lead compounds and improve success rates in the earlier stages of drug discovery.

The guide details the jump-dilution approach to measuring residence time and compares it to other approaches, such as surface plasmon resonance, biolayer interferometry, and resonant acoustic profiling. This article also describes a universal high throughput screening (HTS) compatible assay method broadly applicable to a variety of targets such as kinases, phosphodiesterases (PDEs), and glycosyltransferases (GTFs) using the Transcreener Assay Platform.

The guide provides a step-by-step protocol with examples and case studies that walk a user through the process of both accurately determining resonance time and using a rank order approach amiable to HTS. A comparison of Transcreener’s three fluorescent readouts fluorescence polarization (FP), fluorescence intensity (FI), and TR-FRET gives the researcher multiple options within a suite of drug discovery tools.

In the guide you can discover:

  •     The basics of residence time and its importance to drug discovery
  •     A comparison of methods used for residence time determination
  •     Using the jump-dilution method with Transcreener biochemical assays
  •     Data analysis used to accurately measure residence time
  •     Examples of measuring inhibitor residence time for kinases, PDEs, and GTFs

Please visit bellbrooklabs.com to download the free residence time guide.

About BellBrook Labs:

BellBrook Labs is dedicated to accelerating drug discovery and biological research by providing innovative high throughput screening solutions. BellBrook’s core technology, Transcreener, is a universal, homogenous biochemical assay platform based on detection of nucleotides that makes it easy to screen thousands of different enzymes. These include validated targets like kinases and phosphodiesterases, as well as emerging targets like ATPases, GTPases, methyltransferases, and glycosyltransferases. Detection reagents from BellBrook Labs help researchers progress toward more effective therapies for cancer and other debilitating diseases.

Read the full story at https://www.prweb.com/releases/bellbrook_labs_publishes_a_guide_to_measuring_drug_target_residence_times_with_biochemical_assays/prweb15725311.htm.


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