Compound name
PFI-3
Protein family
Bromodomain
Target name
SMARCA2@BRD
Affinity biochemical (nM)
89
Affinity on-target cellular (nM)
1000
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000199c
SMILES
O=C(/C=C/N1C[C@H]2C[C@@H]1CN2c1ccccn1)c1ccccc1O
InChIKey
INAICWLVUAKEPB-QSTFCLMHSA-N
NCBI gene ID
6595
UniProt ID
P51531
Synonyms
BAF190, hSNF2a, hBRM, Sth1p, SNF2LA, BRM, SNF2, SWI2
Mode of action
Inhibitor
Negative control
PFI-3oMet
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/PFI-3
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
FRAP assay in U2OS cells full-length SMARCA2 protein
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, dTm(PBRM1,BD5) = 9.1 K, dTm(SMARCA2) = 8.2 K, dTM(SMARCA4) = 7.0 K, other targets dTm <1 K; Screened in CEREP panel against 102 cellular receptors and 30 enzymes, closest targets: IC50(A1A) = 0.44 µM, IC50(A1B) = 3.6 µM, IC50(kKOP) = 13 µM, IC50(5-HAT2B) = 4.0 µM;
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.6b00012
Selectivity Number of Off-targets
0