Chemical Probes logo
PF-4800567 | PF-4800567 : ATP competitive inhibitor of CSNK1E
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CSNK1E
  • IC50:32 nM
  • IC50:0.13 uM
ATP competitive
--

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - CSNK1D 711 nM

Potency Assay Off-Target:
In vitro kinase assay; 50 additional kinases were tested at 1 and 1 uM. PF-4800567 inhibited 69% of ...

Potency
Cellular
In Vitro

CSNK1E

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? No

In Vivo Validations

C57BL/J6 mice
Dose: 100 mg/kg
Route of delivery: Subcutaneous
Organ of interest (O): Brain

Reference: --

Chemical Information

Molecular Formula C17H18ClN5O2
SMILEs Nc1ncnc2c1c(COc1cccc(Cl)c1)nn2C1CCOCC1
InChI InChI=1S/C17H18ClN5O2/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21)
Molecular weight 359.11 Da
AlogP 2.992400000000001
HBond acceptors 7
HBond donors 2
Atoms 43

References

Publications

    Cross References

    Vendors

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

    Expert Reviews

    by SERP
    (on 18 May 2016 )
    Cellular Use Rating
    In Model Organisms
    The probe has cellular activity at 2.7 uM, but a target potency of triple-digit nM. Selectivity is ~ 20X at the biochemical level and ~ 10X at the cellular level for CK1d/e. No cellular target-engagement...
    by SERP
    (on 31 May 2016 )
    Cellular Use Rating
    In Model Organisms
    This probe is weakly active in cells (2.7 uM), and mice dosed subcutaneously show only minor effects due to treatment. This probe needs improvement before using in cellular or in vivo models.
    by SERP
    (on 15 Jan 2017 )
    Cellular Use Rating
    This compound also significantly inhibits EGFR.
    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