Compound name
SGC-SMARCA-BRDVIII
Protein family
Bromodomain
Target name
PBRM1@BRD
Affinity biochemical (nM)
13
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001118a
SMILES
OC1=CC=CC=C1C2=CC(N3CCN(C(OC(C)(C)C)=O)CC3)=C(N)N=N2
InChIKey
AQTNUGRRZDRZIA-UHFFFAOYSA-N
NCBI gene ID
55193
UniProt ID
Q86U86
Synonyms
BAF180, PB1
Mode of action
Inhibitor
Negative control
SGC-BRDVIII-NC
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/SGC-SMARCA-BRDVIII
Affinity biochemical relation
0
Selectivity platform
Bromodomain panel (DSF assays)
Selectivity platform number of targets
25
Selectivity remarks
Screened at 20 µM, dTm(SMARCA2) = 7.7 K, dTm(SMARCA4) = 7.4 K, dTm(PBRM1,BD5) = 11.3 K, other targets <2.7 K; Screened at 20 µM against 85 protein kinases (DSF assay), clean selectivity profile with all targets dTm <0.5 K
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/SGC-SMARCA-BRDVIII
Selectivity Number of Off-targets
0