Free PDF: A Guide to Measuring Drug-Target Residence Times with Biochemical Assays

GÖTTINGEN, Germany - Feb. 18, 2020 - PRLog -- During drug development initiatives, analysis of drug-target residence times can improve efficacy, increase therapeutic window, and reduce the risk of premature focus on candidate compounds that are likely to have undesirable side effects. This guide, carefully edited by BellBrook Labs, Madison, WI, USA, provides technical background on concepts and techniques for use of Transcreener® biochemical assays to measure drug-target residence times, along with examples and case studies.

Learn more including:

• 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 determine residence time
• Examples of measuring residence time for kinases, phosphodiesterases, and glycosyltransferases

BellBrook Labs

BellBrook Labs is dedicated to providing the pharmaceutical industry with enabling screening tools to accelerate the discovery of more effective therapies. The proprietary Transcreener® HTS Platform was developed to move more new targets into HTS more rapidly, and to streamline selectivity profiling within a target family. It relies on homogenous fluorescent immunodetection of nucleotides, including ADP, UDP, GDP, AMP and GMP, that are formed by thousands of cellular enzymes. BellBrook is developing microscale cell culture devices with unique advantages for miniaturization and automation of cellular assays: iuvo™ MicroConduit Array Technology. These MicroConduit Arrays rely on liquid displacement from microchannels rather than the cumbersome aspiration and replacement used with open wells, yet they are compatible with existing liquid dispensing equipment.

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