Compound name
BI-9564
Protein family
Bromodomain
Target name
BRD7@BRD
Affinity biochemical (nM)
73
Affinity on-target cellular (nM)
1000
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
29117
UniProt ID
Q9NPI1
Synonyms
CELTIX1, BP75
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