Compound name
GSK8814
Protein family
Bromodomain
Target name
ATAD2
Affinity biochemical (nM)
50.1
Affinity on-target cellular (nM)
2700
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000268b
SMILES
CO[C@H]1CNC[C@@H](OCC2CCC(F)(F)CC2)[C@@H]1Nc1ncc(-c2cncc(C)c2)c2cc(C)c(=O)[nH]c12
InChIKey
YDPMMWAOCCOULO-JBRSBNLGSA-N
Mode of action
Inhibitor
Negative control
GSK8815
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET binding assay
Affinity Biochemical Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201603928
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
NanoBRET assay (truncated ATAD2/histone H3.3)
Affinity on-target cellular source knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201603928
Affinity on-target cellular relation
=
Selectivity platform
BROMOscan (DiscoverX)
Selectivity platform number of targets
37
Selectivity remarks
Clean in BromoScan, > 100 fold selective over TAF1 and TAF1L, enzymatic assay, pKd(TAF1,BD2= 6.7, pKd(TAF1L,BD2) = 6.4; > 1000 fold selective over other bromodomains in the panel;
Selectivity Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201603928
Selectivity Number of Off-targets
0