PFI-7

PFI-7 : Inhibitor of GID4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe PFI-7 is in the process of SERP review.

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Information

GID4

Inhibitor

up to 10 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q8IVV7

Target Class: E3 Ligase

Target SubClass: --

Potency: Kd

Potency Value: 80 nM

Potency Assay: SPR

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Glucose-induced degradation protein 4 homolog, VID ...

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

Uniprot ID: Q8IVV7

Target Class: E3 Ligase

Target SubClass: --

Potency: Activity

Potency Value: 4.1 µM Kdisp

Potency Assay: FP assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Glucose-induced degradation protein 4 homolog, VID ...

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

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

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 data suggests its suitability in biochemical and cell-based assays. A structurally-related negative control compound, PFI-7N, is also available and should be considered when using this probe to interrogate GID4 biology. To date, no in vivo data or broad selectivity panel data have been reported.

(last updated: 27 Apr 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

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). Thus, PFI-7 can be used in biochemical as well as cellular assays. No in vivo data is so far available.

(last updated: 3 May 2022 )