Compound name
TP-472
Protein family
Bromodomain
Target name
BRD9@BRD
Affinity biochemical (nM)
33
Affinity on-target cellular (nM)
320
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000231c
SMILES
CC(=O)c1cc(-c2cc(C(=O)NC3CC3)ccc2C)c2ncccn12
InChIKey
RPBMXJHQYJLPDN-UHFFFAOYSA-N
NCBI gene ID
65980
UniProt ID
Q9H8M2
Synonyms
FLJ13441
Mode of action
Inhibitor
Negative control
TP-472N
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/TP-472
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
Eurofins CEREP Diversity Profiling
Selectivity platform number of targets
96
Selectivity remarks
Screened against 71 receptors and ion channels and against 25 other enzymes at 10 µM, closest targets as % of contr.: Adenosine A1 receptor (14%), Benzodiazepine receptor (47%), PDE2A1 (h) (25%), PDE3A (h) (48%) and PDE4D2 (h) (28%); Selectivity >30 fold over all other bromodomain family members except BRD7: Kd(BRD7) = 340 nM (ITC)
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/TP-472
Selectivity Number of Off-targets
0