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GNE-2861 | Inhibitor of PAK4, PAK5, PAK6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PAK4
  • Ki:PAK4: 3.3 nM
  • EC50:10 uM
PAK5
  • Ki:PAK4: 3.3 nM
  • EC50:10 uM
PAK6
  • Ki:PAK4: 3.3 nM
  • EC50:10 uM
Inhibitor
10-50 uM (see author note in Comments)

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - PAK1: 2.9 uM

Potency Assay Off-Target:
We assessed percentage inhibition at 100 nM using a 222-membered kinase panel (Invitrogen). All exce ...

Potency
Cellular
In Vitro

PAK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

PAK5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

PAK6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Orthogonal Probes def

PF-3758309

Chemical Information

Molecular Formula C22H26N6O2
SMILEs COCCNc1nc2ccc(C#CC3(O)CCCCC3)cc2n1-c1ccnc(N)n1
InChI InChI=1S/C22H26N6O2/c1-30-14-13-25-21-26-17-6-5-16(7-11-22(29)9-3-2-4-10-22)15-18(17)28(21)19-8-12-24-20(23)27-19/h5-6,8,12,15,29H,2-4,9-10,13-14H2,1H3,(H,25,26)(H2,23,24,27)
Molecular weight 406.21 Da
AlogP 2.5027
HBond acceptors 8
HBond donors 4
Atoms 56

References

Publications

    Cross References

    canSARChEMBLBindingDBPDB

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    Expert Reviews

    by SERP
    (on 29 Jun 2017 )
    Cellular Use Rating
    Author's note: GNE-2861 is a potent and exquisitely kinase-selective Group II PAK inhibitor, and to the best of my knowledge, it is the most selective inhibitor for this target group reported in the...
    by SERP
    (on 4 Jul 2017 )
    Cellular Use Rating
    This is the best available probe for group II PAKs (4,5,6). The disconnect between enzyme (PAK4 IC50 8 nM) and cellular effect (effects observed at 10 uM & 50 uM) is highlighted by the authors as surprising...
    by SERP
    (on 4 Nov 2020 )
    Cellular Use Rating
    GNE-2861 is a PAK4/5/6 inhibitor with isoform selectivity over group I PAKs (PAK1/2/3). The binding mode of the inhibitor is well investigated and gives an explanation of the partial isoform selectivity....
    This is a thoroughly characterized probe and the supporting information is of high quality. The disconnect between in vitro and cellular potency, while potentially explicable and consistent with PAK4...

    Author's note

    GNE-2861 is a potent and exquisitely kinase-selective Group II PAK inhibitor, and to the best of my knowledge, it is the most selective inhibitor for this target group reported in the literature. The biochemical...

    (last updated: 29 Jun 2017)

    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