Screening Strategies in Drug Discovery – Multimedia

The requirement for better in-vitro models that are compatible with high-throughput screening campaigns has led to the development of 3D cell cultures models, especially muliticellular spheroids, which retain many of the morphological and genetic traits of tumours.
Here we describe the formation of such spheroids by two methods: on ultra-low attachment plates and in semi-solid agarose. Both methods are compatible with 96- and 384-well microplate formats.

This application note compares the performance of the highest and lowest affinity variants using automated methods and the highly-sensitive bottom reading capabilities of an HTS microplate reader. Sensitive detection of the 22F basal signal allows for use of this variant under a broad range of conditions, providing an assay with both superior dynamic range and sensitivity.

This poster discusses the benefits of comPOUND for automated sample storage and delivery. TTP Labtech’s pneumatic transport technology, lab2lab, integrates these stores with other instrumentation into managed, fully automated workflows, allowing the scientist to focus on research and data analysis.

An attempt to analyze vector-mediated transport properties for the blood-brain barrier choline transporter (BBBCHT) was made to assess and improve drug delivery to the central nervous system.

Support Synergy™ Neo launch by providing speed and sensitivity data for Fluorescence Polarization detection mode in low volume 384-well plate using hERG biochemical assay as a Model.

Demonstration of profiling and primary screening of an epigenetic target; a histone acetylating bromodomain. This is a TR-FRET based application highlighting the use of automated instrumentation and a high-throughput screening (HTS) multi-mode microplate reader.

This application note describes how the Artel MVS® Multichannel Verification System can be used to assess the performance of the liquid handlers integrated into a PerkinElmer cell::explorer high throughput screening (HTS) system.

We have successfully developed a fully automated protocol utilizing a Hamilton MICROLAB STAR integrated with select third party peripheral devices to suit the assay requirements. The method was validated using 23 marketed drugs with diverse physico-chemical properties and a wide range of published apparent permeabilities (Papp).

Growing high-quality protein crystals is still a major bottleneck and very time consuming step in this process. This application note describes screening experiments using the fully automated CyBi®-CrystalCreator in combination with a commercially available crystallization screen from Jena Bioscience.

This research aims to provide proof-in-principle that in silico tools could be applied to public data so as to efficiently identify active chemistry with good ADMET properties.