Chemical Probes logo
CB-5083 | Inhibitor of VCP
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
VCP
  • IC50:11 nM
  • IC50:115–2000 nM
  • EC50:150–800 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - DNAPK 500 nM, PDE6 80 nM

Selectivity Assessment Description:
off target ATPase inhibition 0/175, Kinase inhibition: 1/173; DNAPK (IC50 = 500&nb ...

Potency
Cellular
In Vitro

VCP

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.ccell.2015.10.002

In Vivo Validations

Mouse
Dose: 3 (IV)- 100 (PO) mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 2.83 (IV), 2.56 (PO) h
Systemic clearance: 5.9 (IV) mL/min/kg

DOI Reference: 10.1016/j.ccell.2015.10.002

Negative Control Compounds

cpd 7

Orthogonal Probes def

NMS-873
LC-1028

Chemical Information

Molecular Formula C24H23N5O2
SMILEs Cc1cc2c(C(N)=O)cccc2n1-c1nc2c(c(NCc3ccccc3)n1)COCC2
InChI InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28)
Molecular weight 413.19 Da
AlogP 0.0
HBond acceptors 7
HBond donors 3
Atoms 54

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 13 Sept 2021 )
Cellular Use Rating
In Model Organisms
CB-5083 has been well characterized in terms of its PK profile and cellular activity. In terms of selectivity, it appears to have only been counter-screened in ATPase and kinase panels. The subsequent...
by SERP
(on 23 Sept 2021 )
Cellular Use Rating
In Model Organisms
Choice of concentration is cell-line dependent and is also indication-dependent, most likely. If cytotoxicity is not a desired pharmacological response, using submicromolar concentration may be preferred....
by SERP
(on 11 Oct 2021 )
Cellular Use Rating
In Model Organisms
This is a well-characterized probe recommended for use in cells and in mice. A wide range of biochemical and cellular measurements support a direct effect on VCP/p97. Notably, resistant alleles have...
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. Read more about our evaluation criteria