Compound name
I-BET151 (GSK1210151A)
Protein family
Bromodomain
Target name
BRD4
Affinity biochemical (nM)
790
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000102c
SMILES
COc1cc2c(cc1-c1c(C)noc1C)ncc1nc(O)n([C@H](C)c3ccccn3)c12
InChIKey
VUVUVNZRUGEAHB-CYBMUJFWSA-N
NCBI gene ID
23476
UniProt ID
O60885
Synonyms
HUNKI, MCAP, CAP, HUNK1
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
FP ligand displacement assays
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/21964340/
Affinity biochemical relation
=
Selectivity platform
Bromodomain panel (DSF assays, literature)
Selectivity platform number of targets
26
Selectivity remarks
Screened at 100 µM in DSF assay, closest target: dTm(CEREBBP) = 1-3 K; Screened in CEREP panel against 50 GPCRs, ion channels and transporters at 10 µM, closest target as % inhibition: NK2 (48%)
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/21964340/