Potency assay (off target):
PFI-3 was also profiled against 40 Bromodomains in Tm assay and in BROMOscan assay (DiscoveRx); it had no significant activity against any other Bromodomain.
Probe Selectivity in Vitro:
In a Cerep panel containing 102 cellular receptors and 30 enzymes, PFI-3 had minimal off-target activity, with the most significant IC50s measured against four GPCRs in the micromolar range (alpha1A: 0.4 uM; alpha1B: 3.6 uM; k opioid receptor: 13 uM; 5-HT2B: 4 uM). In a DNA intercalating and unwinding assay, no activity was detected.