GNE-617

GNE-617 : Inhibitor of NAMPT

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe GNE-617 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

NAMPT

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: P43490

Target Class: Enzyme

Target SubClass: Phosphoribosyltransferase

Potency: IC50

Potency Value: 5 nM

Potency Assay: Nampt biochemical inhibition.

PDB ID for probe-target interaction (3D structure): 4KFO

Target aliases:

Nicotinamide phosphoribosyltransferase, PBEF1, PBE ...

DOI Reference: 10.1021/jm4008664

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Assessed for CYP inhibition, GNE-617 shows an IC50 of 200 nM against CYP2C9 (warfarin metabolism assay). No inhibitions (IC50 >10 uM) for other CYP family members (CYP3A4, CYP2D6, CYP1A2, CYP2C19) (DOI: 10.1021/acs.jmedchem.6b00697)

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Single digit nM activity in a range of cell lines. Mouse PK studies indicate good coverage at doses used. Efficacious in U251 human glioblastoma tumor mouse xenograft model at 25 mg/kg PO QDX7. CYP2C9 inhibitor with IC50 of 200 nM

(last updated: 24 Oct 2023 )