Compound name
BI-9564
Protein family
Bromodomain
Target name
BRD9@BRD
Affinity biochemical (nM)
5.9
Affinity on-target cellular (nM)
100
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000004c
SMILES
COc1cc(-c2cn(C)c(=O)c3cnccc23)c(OC)cc1CN(C)C
InChIKey
BJFSUDWKXGMUKA-UHFFFAOYSA-N
NCBI gene ID
65980
UniProt ID
Q9H8M2
Synonyms
FLJ13441
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
Competition binding assay (DiscoverX)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.5b01865
https://www.thesgc.org/chemical-probes/BI-9564
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Recovery After Photobleaching (FRAP) assay U2OS cells
Affinity on-target cellular relation
<
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
48
Selectivity remarks
Screened at 10 µM in DSF assays, dTm(BRD7) = 6.47 K, dTm(BRD9) = 9.21 K, closest target: dTm(CERC2) = 5.61 K, all other bromodomains <2 K; In vitro follow up of closest target: Kd(CERC2, ITC) = 200 nM; Screened against 32 bromodomains at 10 µM (Bromoscan and BromoMax
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.5b01865
Selectivity Number of Off-targets
0