EUB0000208c_EP300@BRD

Chemical structure of compound EUB0000208c
Compound name
SGC-CBP30
Protein family
Bromodomain
Target name
EP300@BRD
Affinity biochemical (nM)
38
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000208c
SMILES
COc1ccc(CCc2nc3cc(-c4c(C)noc4C)ccc3n2C[C@H](C)N2CCOCC2)cc1Cl
InChIKey
GEPYBHCJBORHCE-SFHVURJKSA-N
NCBI gene ID
2033
UniProt ID
Q09472
Synonyms
p300, KAT3B
Mode of action
Inhibitor
Negative control
BDOIA513
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://doi.org/10.1073/pnas.1501956112
https://www.thesgc.org/chemical-probes/CBP30
Affinity biochemical relation
=
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM in DSF assay, dTM (CREBBPA/EP300A) = 9.6/ 10.4 K, closest targets: dTM(BRD4) = 2.0 K, dTM(BRD3) = 1.9 K, dTm(BRD2) = 1.4 K, dTm (BRD3) = 1.2 K; Follow-up Kds via ITC: Kd(BRD4 at BD1/ BD2) = 0.854/ 4.88 µM, Ki(BRD3 at BD1/ BD2) = 1.09/ 2.19 µM, Kd(BRD2 at BD1/BD2) = 1.01/ 1.76 µM, Kd(BRD3 at BD1/BD2) = 1.09/ 2.19µM; Screened in CEREP panel against 104 receptors, ion channels and other enzymes, closest targets: Ki(alpha2A) = 570 nM, Ki(alpha2C) = 110 nM, Ki(PAF) = 540 nM;
Selectivity Source Knowledge
https://doi.org/10.1073/pnas.1501956112
https://www.thesgc.org/chemical-probes/CBP30
Selectivity Number of Off-targets
0