Screening Strategies in Drug Discovery – Multimedia

Poster
Intelligent K-Means Clustering in a Multiple Endpoint Environment
The main success of QSAR predictive technology is mainly related to the modelling of the single activity/property endpoint in chemical space. Unfortunately an optimisation of the targeted endpoint may result in losing other desired properties, for example, toxicity is increased or solubility reduced. Because of this, attempts have been made in the last few years to model chemical space against multiple endpoints.

Poster
Use of Nanolitre Pipetting in Hit-to-Lead Optimisation
Assay-ready plates are becoming key to maximizing throughput for many HTS departments. These plates contain test compounds prepared from library stocks ahead of time at the correct concentrations. DMSO is routinely used for compound dissolution, but its presence at concentrations above 1% can markedly affect assay performance. Thus, accurate nanolitre quantities of DMSO-based stock solution are required to keep concentrations low when preparing assay-ready plates.

Poster
High Throughput High Content Screening using a Multiwavelength Microplate Cytometer
The Acumen eX3, a multiwavelength microplate cytometer, offers 405, 488 and 633 nm laser excitations in one instrument. This advancement significantly extends the range of fluorescent reagents that can be combined in multicolour, multiplexed assays over a wavelength range for excitation that is similar to that of white light source instrumentation. Thus, it permits seamless transfer of high content assay protocols, developed using CCD-based imaging devices, onto the Acumen eX3 for screening.

Poster
A Total Solution to Provide High Content Primary and Secondary Screening of a Compound Library
TTP LabTech recently published a novel approach using the Acumen Explorer with Invitrogen’s GeneBLAzer technology to measure GPCR activation in cell-based assays. This is multiplexed with a cytotoxicity readout to reduce false positives commonly identified in bulk fluorescence assays. TTP LabTech and Velocity11 have designed a fully automated, single platform using this assay to perform both primary and hit-confirmation screens on a 400,000 compound library in only one week.

Poster
An Ultra-High Throughput Approach to High Content Screening in 1536-Well Format
The Acumen Explorer combines the object-recognition capabilities of image-based systems with read speeds similar to that of bulk readers. Here, we demonstrate the powerful integration of an Acumen Explorer with the Kalypsys® Integrated Screening System, with capability to screen > 300,000 wells per day of high content data.

Poster
Comparative Virtual and Experimental High-Throughput Screening for Glycogen Synthase Kinase-3b Inhibitors
Glycogen synthase kinase-3b (GSK-3b ) is a serine/threonine kinase that has recently emerged as a key target for neurodegenerative diseases and diabetes. As an initial step of our lead discovery program we developed a virtual screen to discriminate known GSK-3b inhibitors and inactive compounds using FlexX, FlexX-Pharm and FlexE.

Poster
NanoQuot™, A Cost-Effective, Flexible Nanoliter Dispenser for High Throughput Screening
BioTek has developed the NanoQuot™, a dispenser capable of running stand-alone or computer controlled as part of a robotics system. Positive gas pressure system, in conjunction with eight precision valves, provides accurate and precise dispensing of volumes ranging from 100 nanoliters to 40 microliters in 96-, 384-, and 1536-well plates.

Poster
A new High Content Screening Paradigm: Combination of Image Analysis Software and Microplate Cytometry
Researchers are under increasing pressure to perform high content cell-based assays at throughputs compatible with primary screening. Where throughput is not an issue, microscope-based CCD imagers have predominated within the high content field, due to the breadth of biological assays that can be addressed by image analysis techniques. However, they have limited utility for screening due to their low throughput, limited field of view and generation of terabytes of image data.

Poster
The Synergy™ 2, A Novel Approach to Microplate Multi- Detection for HTS and Drug Discovery
The Synergy™ 2 is a new type of reader that provides research laboratories with performances usually found on high-end HTS instrumentation, while delivering flexibility and efficient cost-control to screening laboratories. The Synergy 2 utilizes multiple optics to provide performance regardless of the detection technology.

Poster
Achieving Ultra High Performance Screening
High throughput (HT) and Ultra High Throughput (UHT) screening remains a valuable and necessary approach to modern drug discovery. Successful application of HTS requires accurate and meaningful handling of the experimental results. This means capturing vast data volumes generated by HTS and UHTS programmes and subsequent validation and verification. Decision making regarding HTS data can be supported via comprehensive and intuitive visualization of results.
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