Compound name
PFI-4
Protein family
Bromodomain
Target name
BRPF1@BRD
Affinity biochemical (nM)
13
Affinity on-target cellular (nM)
242
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000224e
SMILES
COc1ccccc1C(O)=Nc1cc2c(cc1N1CCCC1)n(C)c(=O)n2C
InChIKey
QCIJLRJBZDBVDB-UHFFFAOYSA-N
NCBI gene ID
7862
UniProt ID
P55201
Synonyms
BR140
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/PFI-4
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
48
Selectivity remarks
Screened in DSF assay at 10 µM, closest target: dTm(CECR2) = 2 K, follow up in Alpha Screen: IC50(CECR2) = 2.32 µM
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/PFI-4
Selectivity Number of Off-targets
1