Compound name
GSK6853
Protein family
Bromodomain
Target name
BRPF1@BRD
Affinity biochemical (nM)
7.9
Affinity on-target cellular (nM)
20
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000224d
SMILES
COc1ccccc1C(=O)Nc1cc2c(cc1N1CCCC1)n(C)c(=O)n2C
InChIKey
QCIJLRJBZDBVDB-UHFFFAOYSA-N
NCBI gene ID
7862
UniProt ID
P55201
Synonyms
BR140
Mode of action
Inhibitor
Negative control
GSK9311
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acsmedchemlett.6b00092
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
BROMOscan™ panel (DiscoverX)
Selectivity platform number of targets
35
Selectivity remarks
>1600-fold selective, closest targets: pKd(BRPF2/BRD2) = 6.29, pKd(BRPF3) = 6.00, pKd(BRD9) = 6.00, pKd(BRD7) = 6.09; Screened against 48 ion channels, GPCRs and other enzymes, all pXC50 <5, compound is highly selective;
Selectivity Source Knowledge
https://doi.org/10.1021/acsmedchemlett.6b00092
Selectivity Number of Off-targets
0