Compound name
GSK943
Protein family
Bromodomain
Target name
BRD4@BD2
Affinity biochemical (nM)
7943
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001134a
SMILES
CNC(=O)c1cc(C(=O)N[C@@H]2[C@H]3COC[C@H]32)cc2c1O[C@@H](CF)[C@@H]2c1ccccc1
InChIKey
WZQLVEPIBAOOGF-PXTPFGJHSA-N
NCBI gene ID
23476
UniProt ID
O60885
Synonyms
HUNKI, MCAP, CAP, HUNK1
Mode of action
Negative control for GSK973
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/chemProbes#!specificprobeoverview/GSK973
Affinity biochemical relation
0
Selectivity platform
GPCR panel (PDSP screen)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, in-vitro potency of closest target: Ki(GABA/BZP) = 473.91 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/GSK973
Selectivity Number of Off-targets
0