KINOMEscan™ Binding Assays by DiscoveRx Corporation

The KINOMEscan screening platform employs a novel and proprietary active site-directed competition binding assay to quantitatively measure interactions between test compounds and more than 450 kinase assays and disease relevant mutant variants. This robust and reliable assay technology affords investigators the ability to extensively annotate compounds with accurate, precise and reproducible data. KINOMEscan assays do not require ATP and thereby report true thermodynamic interaction affinities, as opposed to IC50 values, which can depend on the ATP concentration.

KINOMEscan Platform Benefits & Features:

• Rapid turnaround time Largest commercially available kinase assay panel
• Flexible: screen any number of compounds against any number of kinases
• Custom panel capabilities to support ongoing drug discovery programs
• High throughput: >4000 compounds per month screened across full panel (>1.7 million interactions)
• Accurate affinity (Kd) measurements from 10 uM ATP not required: delivers true thermodynamic affinity data as opposed to IC50s
• Includes clinically relevant catalytically inactive pseudokinases (e.g. ERBB3)
• Includes activation state-specific assays that provide inhibitor binding mode information
• No interference from compound fluorescence
• All assays performed in parallel under standardized conditions as a single experiment
• Accurate, precise, reproducible data