BAY-885 | Inhibitor of MAPK7
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
In Vivo

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAPK7
  • IC50:35 nM (@250 uM ATP)
  • IC50:115 nM
Inhibitor
1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity against Eurofins kinase panel at 1 μM (350 kinases were tested). Residual kinase acti ...

Potency
Cellular
In Vitro

MAPK7

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Negative Control Compounds

BAY-693

Orthogonal Probes def

AX15836
XMD8-92

Chemical Information

Molecular Formula C25H28F3N7O2
SMILEs CN1CCN(c2cnc3c(C4CCN(C(=O)c5ccc(OC(F)(F)F)cc5N)CC4)ncnc3c2)CC1
InChI InChI=1S/C25H28F3N7O2/c1-33-8-10-34(11-9-33)17-12-21-23(30-14-17)22(32-15-31-21)16-4-6-35(7-5-16)24(36)19-3-2-18(13-20(19)29)37-25(26,27)28/h2-3,12-16H,4-11,29H2,1H3
Molecular weight 515.23 Da
AlogP 3.2772000000000023
HBond acceptors 9
HBond donors 2
Atoms 65

References

Publications

    Vendors

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

    Expert Reviews


    (on 22 May 2020 )
    Cellular Use Rating
    BAY-885 is an excellent inhibitor of ERK5. It is potent, selective against other kinases and bromodomain-containing proteins, and active in cells. There is not an inactive close analogue that is commercially...
    (on 4 Jul 2020 )
    Cellular Use Rating
    1 uM is a reasonable maximum concentration to ensure ERK5 inhibition while not perturbing many other kinases. However, care should be taken in phenotypic assays to rule out inhibition of FER and ephrin...
    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