CREBBP NanoBRET Bromodomain Histone Interaction

CBP/Histone 3.3 NanoBRET Protein Protein Interaction Assay in Living Cells

Target Overview

Target

CREBBP/Histone 3.3

HGNC Symbol

CREBBP/H3-3A

Synonyms

CREBBP: CBP, CBP-BD, CREB binding protein, RSTS, RTS, CBP, KAT3A
Histone H3.3: H3F3, H3F3A, H3.3A

Cell Line

HEK293 human epithelial cell line from ATCC

Assay Properties

Assay Format

NanoBRET Bromodomain Histone Interaction

Assay Protocol

HEK293 cells were transfected with Histone H3.3-HaloTag Fusion Vector DNA plus CREBBP-BD-NanoLuc vector. The transfected cells were pre-treated with NanoBRET^TM 618 Ligand and then treated with reference compound SGC-CBP-30 (starting at 10 uM, 10-dose with 3-fold dilution) for 22 hours. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism program based on a sigmoidal dose response equation.

Readout

384-well plate format using Promega’s NanoBRET Assay

Reference Compound IC50s

Compounds	IC50 (µM)
SGC-CBP-30	2.268

Screening Location

Malvern, USA