| Assay Method Information | |
| | In Vitro Activity Against CBP |
| Description: | The potency and selectivity of CBP/P300 inhibitor compounds including 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 uM to 1.7 nM. 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. In these conditions, Compound 1 was determined to be a potent inhibitor of CBP with an IC50<2 nM (N=16). In a similar assay, BRD4 potency was determined and Compound 1 showed an IC50 of <500 nM (N=15), indicating >200-fold selectivity. |
| Affinity data for this assay | |
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