Compound name
GSK620
Protein family
Bromodomain
Target name
BRD3@BD2
Affinity biochemical (nM)
79
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001117a
SMILES
CNC(C1=CC(=CN(Cc2ccccc2)C1=O)C(NC1CC1)=O)=O
InChIKey
QZZCUOVXHPAQRQ-UHFFFAOYSA-N
NCBI gene ID
8019
UniProt ID
Q15059
Synonyms
RING3L, ORFX, KIAA0043
Mode of action
Inhibitor
Negative control
No control available for probe
Affinity biochemical definition
IC50
Affinity biochemical assay type
BET mutant TR-FRET assay (BD2)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/GSK620
Affinity biochemical relation
0
Selectivity platform
BROMOScan (DiscoverX)
Selectivity platform number of targets
40
Selectivity remarks
In-vitro potencies of closest targets in BROMOScan (DiscoverX): pKd(TAF1, BD2) = 5.4, pKd(EP300) = 5.1, pKd(CREBBP) = 5.0, pKd(EP300) = 5.1; Cross screening in liability panel against 48 targets (GPCRs, transporter, ion-channels, and other targets), closest target: pEC50(CB2 receptor) <5; Selective for BD2 domain of BET proteins; Screened at 10 µM against 45 GPCRs (PDSP screen), closest target as % inhibition: OPRK1(40%);
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/GSK620
Selectivity Number of Off-targets
0