, Antagonist of EP300, CREBBP
In Vitro Validations
Uniprot ID: Q09472
Target Class: Epigenetic
Target SubClass: Bromodomain
Potency Value: 47 nM
Potency Assay: Biolayer interference.
PDB ID for probe-target interaction (3D structure): 5BT3
Histone acetyltransferase p300, P300, EP300, EP300 ...
DOI Reference: 10.1073/pnas.1501956112
In Cell Validations
In Vivo Data
No in Vivo Validations
Off-Target Selectivity Assesments
Potency assay (off target): DSF binding assay
Probe Selectivity in Vitro:
In DSF binding assays with 45 bromodomains, SGC-CBP30 had no significant activity except against BRD2, BRD3, and BRD4. SGC-CPB30 had minimal activity against 136 GPCRs, ion channels, enzymes, and kinases with IC50s >1 uM, except Adrenergic receptor alpha 2C (0.11 uM), alpha 2A (0.57 uM), PDE5 (0.15 uM), and PAF (0.51 uM).
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