| 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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