EUB0000256b_KAT2A@BRD

Chemical structure of compound EUB0000256b
Compound name
GSK4027
Protein family
Bromodomain
Target name
KAT2A@BRD
Affinity biochemical (nM)
1.4
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000256b
SMILES
CN1C[C@H](Nc2cnn(C)c(=O)c2Br)C[C@H](c2ccccc2)C1
InChIKey
VZAFGXCWAWRULT-UONOGXRCSA-N
NCBI gene ID
2648
UniProt ID
Q92830
Synonyms
GCN5, PCAF-b
Mode of action
Inhibitor
Negative control
GSK4028
Affinity biochemical definition
Ki
Affinity biochemical assay type
Bromoscan assay(DiscoverX)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.6b01566
https://www.thesgc.org/chemical-probes/GSK4027
Affinity biochemical relation
=
Selectivity platform
BROMOscan panel (DiscoverX)
Selectivity platform number of targets
34
Selectivity remarks
Closest targets: Ki(BRPF3) = 100 nM, Kd(BRD1) = 110 nM, Kd(FALZ) = 130 nM, Kd(BRPF1) = 140 nM, Kd(BAZB) = 840 nM, Kd(BRD7) = 1500 nM, Kd(BRD9) = 1400 nM, others >20 µM; Screened against 50 receptors, ion channels and other enzymes (internal GSK panel), closest target: XC50(AChEase) = 3.2 µM, others >4 µM
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.6b01566
Selectivity Number of Off-targets
1