| Assay Method Information | |
| | In Vitro Activity Against CBP |
| Description: | The potency and selectivity of CBP/P300 inhibitor compounds including Compound 1 and Compound 1'were determined in biochemical time resolved fluorescence assays using GST fusions of the bromodomains of CBP and BRD4. Briefly, CBP inhibitors were pre-dispensed into 1536 assay plates for a final test concentration of 33 μM to 1.7 nM. Protein and Ligands were added to the compound to a final concentration of 2.5 nM CBP or BRD4 (N-terminal GST-CREBBP (1081-1197), BRD4 tandem domains) and 25 nM Tetra-Acetylated H3 peptide Plates and incubated for 4 h. Data were reported as percent inhibition compared with control wells. IC50 values were determined by curve fitting of the standard 4 parameter logistic fitting algorithm. |
| Affinity data for this assay | |
|---|---|
| If you find an error in this entry please send us an E-mail | |