Compound name
BAZ2-ICR
Protein family
Bromodomain
Target name
BAZ2B@BRD
Affinity biochemical (nM)
170
Affinity on-target cellular (nM)
1000
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000192d
SMILES
Cn1cc(CCn2cnc(-c3cnn(C)c3)c2-c2ccc(C#N)cc2)cn1
InChIKey
RRZVGDGTWNQAPW-UHFFFAOYSA-N
NCBI gene ID
29994
UniProt ID
Q9UIF8
Synonyms
WALp4
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/jm501963e
https://www.thesgc.org/chemical-probes/BAZ2-ICR
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
FRAP assay (utilizing GFP-tagged BAZ2A full length protein transfected into U2OS cells)
Affinity on-target cellular relation
<
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
47
Selectivity remarks
Screeed at 10 µM in thermal shift assays, dTm(BAZ2A) = 5.2 K, dTm(BAZ2B) = 3.8 K, dTm(CECR2) = 2.0 K; Follow-up in vitro potency (ITC): Kd(CECR2) = 1.55 µM (15-fold selective); Greater 100-fold selective for BRD4 (IC50 >50 µM, BRD4 AlphaScreen assay); Clean profile in CEREP screen against 55 targets (receptors, ion chanels) at 10 µM;
Selectivity Source Knowledge
https://doi.org/10.1021/jm501963e
Selectivity Number of Off-targets
1