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PFI-7 | PFI-7 : Inhibitor of GID4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GID4
  • Kd:80 nM
  • Activity:4.1 µM Kdisp
  • EC50:600 nM
Inhibitor
up to 10 uM

Selectivity

Potency
Cellular
In Vitro

GID4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-024-01618-0

Negative Control Compounds

CANSAR3550545
Notes: PFI-7N Kd = 5000 nM (SPR)

Chemical Information

Molecular Formula C24H27N5O
SMILEs O=C(CNCc1cc2ccccc2[nH]1)N[C@H]1CC[C@@H](c2nc3ccccc3[nH]2)CC1
InChI InChI=1S/C24H27N5O/c30-23(15-25-14-19-13-17-5-1-2-6-20(17)26-19)27-18-11-9-16(10-12-18)24-28-21-7-3-4-8-22(21)29-24/h1-8,13,16,18,25-26H,9-12,14-15H2,(H,27,30)(H,28,29)/t16-,18+
Molecular weight 401.22 Da
AlogP 0.0
HBond acceptors 6
HBond donors 4
Atoms 57

Expert Reviews

by SERP
(on 27 Apr 2022 )
Cellular Use Rating
PFI-7 is a potent inhibitor of GID4 (Kd = 80 nM) developed by scientists at Pfizer and SGC. Cellular target engagement has been obtained using a NanoBRET assay (EC50 = 600 nM) in HEK293T cells. These...
by SERP
(on 3 May 2022 )
Cellular Use Rating
PFI-7 binds to GID4 in SPR assays (KD = 80 nM). Furthermore, the Pfizer team has shown in cell-based NanoBRET assays that PFI-7 can displace a known degron peptide from full-length GID4 (EC50 = 600 nM)....
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