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Introduction	Application Presentations	References

Label-free screening

High quality screening data increases productivity and cost-efficiency:

	•	Efficiently eliminates false-positives (easy provision of selectivity controls)
	•	Enables screening of problem targets with unknown or unstable substrates (direct compound-target binding assays)
	•	In-built quality contol of data - poor compound behavior evident as binding artifacts in real-time interaction curves
	•	Low consumption of target proteins compared to alternative methods

"The multi-target protein panel approach in Biacore A100 is an excellent way to study complex drug targets and the chance to find biological activity is enhanced when performing these assays as the information obtained gives a clear picture on the mode of binding."
Dr. Walter Huber, F. Hoffman La-Roche, Basel, Switzerland.

Screening applications in early drug discovery

High quality data on the selective binding of LMW compounds to a target protein enable more confident selection of hit compounds during the early stages of drug discovery. Label-free interaction analysis provides this data, enabling primary screening of smaller, focused libraries, or screen-to-hit confirmation downstream of high throughput screening (HTS) assays:

Primary screening of fragment libraries in structure-based approaches

	•	Invaluable pre-selection of binders prior to expensive crystallographic analysis
	•	Provides sensitivity required for detection of low-affinity binding of very low MW fragments
	•	Low target-consumption analysis confidently identifies fragment subset for demanding structural studies

Secondary screening/ hit confirmation in HTS workflows

	•	Sensitive, high quality binding data with selectivity controls - efficiently eliminate false positives and negatives
	•	Affinity ranking of hit compounds
	•	1:1 binding analysis and binding site information

Compounds from a virtual screening library directed against a trimeric protein target (Roche, Basel) were screened simultaneously against full-length and a-subunit proteins. Rapid identification of compounds with selectivity for the full-length trimer compared to the a-subunit. Compound binding to the two target proteins was compared using a scatter plot (240 of the 1280 total compounds shown).

_{(Data courtesy of Dr. Walter Huber, Roche, Basel)}

Biacore A100 was used to screen multiple replicates of 560 compounds from a commercial library against multiple serum albumins from several different species. Around 8000 wells were screened against the target panel (i.e. 30 000 interactions) in just a few weeks. Reproducibility of reference Warfarin controls was excellent (SD = 1.2 RU, or 5%) and weak binders were readily distinguished from negative controls. This ADME panel screening approach readily identifies compounds with significant species selectivity for albumin, information that offers valuable risk assessment for ADME studies in animal models.

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Biacore A100
Unmatched productivity

	•		Identify selective binders using informative panels of target proteins for successful drug discovery
	•		Screening of fragment libraries for pre-selection of binders prior to demanding structural studies