PFI-653

2D structure
Target VNN1 
Targeted domain Near catalytic site
Mode of action Inhibitor
Control PFI-653-N
Recommended cellular usage concentration ≤ 1 µM
In vivo use Yes
Synonyms Vanin-1-IN-1
Donated by Pfizer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Human recombinant VNN1 assay with 25 pM VNN1: IC50 = 6.85 nM; Mouse VNN1: IC50 = 24.5 nM
Selectivity within target family: > 30-fold Nitrilase family selectivity: BTD (Biotinidase): IC50 > 50 µM (>7000 fold)
Selectivity outside target family Protease panel (Reaction Biology Corp.) (63 proteases) at 1 µM: all < 10 % inhibition
Invitrogen kinase panel (483 kinases) at 1 µM and Km ATP: all < 30 % inhibition
CEREP panel (66 enzymes, receptors, and ion channels) at 10 µM: all < 25 % inhibition
PDE panel: all IC50 >30 µM
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Human plasma VNN1 assay with 8 nM VNN1: IC50 = 9.0 nM ; Mouse plasma VNN1: IC50 = 53.4 nM; Rat plasma VNN1: IC50 = 12 nM
Control compound (100 times less potent than the probe) PFI-653-N: Human VNN1 assay: IC50 > 17.6 µM
Human plasma VNN1 assay: IC50 > 3 µM