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GNE-617 | GNE-617 : Inhibitor of NAMPT
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NAMPT
  • IC50:5 nM
  • IC50:2 nM
  • IC50:1.8-7.4 nM
  • EC50:1.1 nM
  • EC50:1.3 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Assessed for CYP inhibition, GNE-617 shows an IC50 of 200 nM against CYP2C9 (warfarin metabolism ass ...

Potency
Cellular
In Vitro

NAMPT

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm4008664

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intravenous
Systemic clearance: 52.4 mL/min/kg
Volume of Distribution at Steady-State: 6.7 L/kg

DOI Reference: 10.1021/jm4008664

Dose: 10 mg/Kg
Route of delivery: Oral
Cmax: 1.21 uM
Tmax: 0.25 h
Area Under the Curve:: 3.06 μM*h
Bioavailability: 41.1%

DOI Reference: 10.1021/jm4008664

Chemical Information

Molecular Formula C21H15F2N3O3S
SMILEs O=C(NCc1ccc(S(=O)(=O)c2cc(F)cc(F)c2)cc1)c1ccc2nccn2c1
InChI InChI=1S/C21H15F2N3O3S/c22-16-9-17(23)11-19(10-16)30(28,29)18-4-1-14(2-5-18)12-25-21(27)15-3-6-20-24-7-8-26(20)13-15/h1-11,13H,12H2,(H,25,27)
Molecular weight 427.08 Da
AlogP 3.375300000000002
HBond acceptors 6
HBond donors 1
Atoms 45

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 24 Oct 2023 )
Cellular Use Rating
In Model Organisms
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...
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