| Assay Method Information | |
| | LanthaScreen® Eu Kinase Binding Assay |
| Description: | In vitro binding of the compounds to the ATP pocket of CDK8 in complex with Cyclin C was carried out by LanthaScreen® Eu Kinase Binding Assay based on the binding and displacement of a proprietary, Alexa Fluor® 647-labeled, ATP-competitive kinase inhibitor scaffold (kinase tracer) to the kinase of interest. The binding of the tracer to the kinase is detected using a europium-labeled anti-tag antibody, which binds to the kinase of interest. Simultaneous binding of both the tracer and antibody to the kinase results in a high degree of FRET (fluorescence resonance energy transfer) from the europium (Eu) donor fluorophore to the Alexa Fluor® 647 acceptor fluorophore on the kinase tracer. The binding of an inhibitor to the kinase competes for binding with the tracer, resulting in a loss of FRET. |
| Affinity data for this assay | |
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