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GSK8612 | GSK8612 : Inhibitor of TBK1
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
TBK1
  • Kd:10 nM
  • IC50:1000 nM
  • IC50:800 nM
  • IC50:500 nM
Inhibitor
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
closest off-targets were STK17B and IKKepsilon with >> 50 fold selectivity
Selectivity Assessment Description:
Chemoproteomics based kinase selectivity of GSK8612 determined using kinobeads in mixed HEK293, K-56 ...

Potency
Cellular
In Vitro

TBK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.9b00027

Orthogonal Probes def

1FV
BX-795

Chemical Information

Molecular Formula C17H17BrF3N7O2S
SMILEs Cc1nn(CC(F)(F)F)cc1Nc1ncc(Br)c(NCc2ccc(S(N)(=O)=O)cc2)n1
InChI InChI=1S/C17H17BrF3N7O2S/c1-10-14(8-28(27-10)9-17(19,20)21)25-16-24-7-13(18)15(26-16)23-6-11-2-4-12(5-3-11)31(22,29)30/h2-5,7-8H,6,9H2,1H3,(H2,22,29,30)(H2,23,24,25,26)
Molecular weight 519.03 Da
AlogP 3.309420000000001
HBond acceptors 9
HBond donors 4
Atoms 48

References

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Cross References

canSARChEMBLBindingDB

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Expert Reviews

by SERP+
(on 23 May 2024 )
Cellular Use Rating
GSK8612 is a highly potent ATP-competitive inhibitor of TBK1 (Kd = 10 nM in kinobeads in vitro assay), with an approx. 10-fold higher affinity for the inactive state of the protein kinase (Kd in cell extracts...
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