Compound name
PFI-1
Protein family
Bromodomain
Target name
BRDT@BD2
Affinity biochemical (nM)
220.8
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000322b
SMILES
CN1Cc2cc(ccc2NC1=O)NS(c1ccccc1OC)(=O)=O
InChIKey
TXZPMHLMPKIUGK-UHFFFAOYSA-N
NCBI gene ID
676
UniProt ID
Q58F21
Synonyms
BRD6, CT9
Mode of action
Inhibitor
Negative control
No control available for probe
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://aacrjournals.org/cancerres/article/73/11/3336/584303/PFI-1-a-Highly-Selective-Protein-Interaction
Affinity biochemical relation
0
Selectivity platform
Bromodomain panel (DSF assays)
Selectivity platform number of targets
42
Selectivity remarks
Screened in DSF assays, dTm values of closest targets: dTm(EP300) = 2.71 K, dTm(CREBBP) = 2.66 K, dTm of main targets: dTm(BRD2, BD1) = 4.61 K, dTm(BRD2, BD2) = 5.32 K, dTm(BRD3, BD1) = 5.24 K, dTm(BRD3, BD2) = 5.45 K, dTm(BRD4, BD1) = 6.84 K, dTm(BRD4, BD2) = 3.79 K, dTm(BRDT, BD1) = 2.08 K; Screened at 1 µM against 38 protein kinases (Invitrogen kinase panel), closest targets as % of inhibition: NTRK1 (28.5%), CHEK1 (16%); Screened at 10 µM against 14 membrane receptors, closest targets as % of inhibition: PDE3B (46.3%), H1 (6.5%)
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/PFI-1
Selectivity Number of Off-targets
0