Compound name
OF-1
Protein family
Bromodomain
Target name
BRPF3@BRD
Affinity biochemical (nM)
2406
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000323b
SMILES
COC1=CC(N2C)=C(C=C1NS(=O)(C3=CC=C(C=C3C)Br)=O)N(C)C2=O
InChIKey
YUNQZQREIHWDQT-UHFFFAOYSA-N
NCBI gene ID
27154
UniProt ID
Q9ULD4
Synonyms
KIAA1286
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acschembio.7b00481
https://www.thesgc.org/chemical-probes/OF-1
Affinity biochemical relation
=
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
49
Selectivity remarks
Screened in DSF-panel, closest target: dTm(BRD4, BD1) = 2.1 K; In vitro follow-up with AlphaScreen: IC50(BRD4, BD1) >10 µM, ITC: Kd(BRD4, BD1) = 3.9 µM; Screened in CEREB panel against 56 GPCRs, ion channels and transporters at 10 µM, closest targtes as % inhibition: A1 (82%), 5-HT6 (54%), A3 (53%);
Selectivity Source Knowledge
https://doi.org/10.1021/acschembio.7b00481
Selectivity Number of Off-targets
1