Compound name
(+)-JQ1
Protein family
Bromodomain
Target name
BRD2@BD1
Affinity biochemical (nM)
128.4
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000330a
SMILES
O=C(C[C@@H]1N=C(C2=C(N3C1=NN=C3C)SC(C)=C2C)C4=CC=C(C=C4)Cl)OC(C)(C)C
InChIKey
DNVXATUJJDPFDM-KRWDZBQOSA-N
NCBI gene ID
6046
UniProt ID
P25440
Synonyms
KIAA9001, RING3, D6S113E, NAT, FSRG1
Mode of action
Inhibitor
Negative control
(-)-JQ1
Affinity biochemical definition
Kd
Affinity biochemical assay type
Isothermal titration calorimetry (ITC)
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/nature09504
https://www.thesgc.org/chemical-probes/JQ1
Affinity biochemical relation
=
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
37
Selectivity remarks
Screened at 10 µM in DSF-assay, closest target: dTM(CREBBP) = 1.04 K, inactive in CEREP assay; Screened at 1 µM in CEREP panel against 55 ligand receptors, ion channels and transporters, clean profile;
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/JQ1
Selectivity Number of Off-targets
0