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Introduction	Application Presentations	References

Label-free characterization

Fast, well-informed decisions are essential to identify, as early as possible, candidates with the highest chance of success. Comprehensive characterization using label-free interaction analysis provides multiple parameters upon which to base such decisions:

	•	selectivity of binding
	•	ranking of target binding affinities
	•	detailed characterization of binding kinetics
	•	SAR/QSAR
	•	thermodynamics
	•	early in vitro ADME indications (plasma protein binding, liposome absorption)
	•	binding site studies

Compound characterization applications in drug discovery & development

Comprehensive characterization of the interaction of LMW compounds with a target protein is extremely important during the stages where hundreds of potential 'lead compounds' must be investigated before subsequent optimization of selected leads.

"The analysis provided crucial kinetic information that enabled a much more informed assessment of the lead series compounds than would have otherwise been possible."
Phillip Debnam, PhD, Senior Scientist, Avidex Ltd, Oxford, UK.

On/off-rate map of compounds from five lead series (Avidex Ltd). Compounds in the yellow-shaded region would have been discarded based on their moderate affinities, but were kept in development due to their very slow off-rates, as determined using label-free interaction analysis.

Early in vitro ADME using label-free compound characterization provides useful indicators of PK-related properties. Compounds were ranked according to their interactions with liposomes of different compositions (and hence, charge properties) that were captured on a lipophilic sensor surface. The 2D plot shows compound binding levels to Aventi blend and POPC liposomes, indicating the good general correlation with published fraction absorbed (Fa) values.

Confident candidate selection and lead optimization increases productivity and cost-efficiency:

	•	Facilitates compound selection by providing best quality, high information content binding data
	•	Enables characterization of compound properties related to efficacy and safety early in the discovery process (assay flexibility)
	•	Enables analysis of problem targets with unknown or unstable substrates (direct compound-target binding assays)
	•	Consumes low amounts of target proteins compared to alternative methods

Which system should I choose?

Good

Better

Best

Biacore T100
Unmatched performance

	•		Develop assays to characterize target: LMW compound interactions
	•		Characterize critical binding properties to facilitate compound selection - affinity, kinetics and thermodynamics

Biacore A100
Unmatched productivity

	•		Identify selective binders using informative panels of target proteins for successful drug discovery
	•		Characterize key binding properties (e.g. affinity and kinetics) with maximum productivity
	•		Maximize information on compound behavior using multiplex, parallel analysis assays