NanoBRET TE Intracellular BET BRD Complete Kit

The NanoBRET Target Engagement (TE) Intracellular BET BRD Assay measures compound binding at select BET bromodomain target proteins within intact cells. This target engagement assay is based on the NanoBRET System, an energy transfer technique designed to measure molecular proximity in living cells. The NanoBRET TE BET BRD Assay analyzes the apparent affinity of test compounds by competitive displacement of a NanoBRET tracer reversibly bound to a NanoLuc BET BRD fusion protein in cells. The NanoBRET TE Assay uses four key components: An expressed cellular target protein that is fused to the bright NanoLuc luciferase; a cell-permeable fluorescent tracer that specifically binds to the target protein; a substrate for NanoLuc luciferase; and a cell-impermeable inhibitor for NanoLuc luciferase. Bioluminescence resonance energy transfer (BRET) is achieved by transferring the luminescent energy from NanoLuc luciferase to the fluorescent tracer that is bound to the target protein-NanoLuc fusion. Compounds that are applied to the cells and specifically engage the intracellular target protein-NanoLuc fusion will result in a decrease in BRET. To ensure accurate assessment of intracellular target engagement, a NanoLuc inhibitor is used to mitigate any extracellular NanoLuc signal that may arise from cells compromised during handling, while not adversely affecting NanoLuc luciferase expressed within healthy living cells. For more details on NanoBRET technology and a full list of available NanoBRET Target Engagement Assays visit: