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GSK2334470 | GSK2334470 : Type I Inhibitor of PDPK1
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
PDPK1
  • IC50:2.5 nM
  • IC50:113 nM
Inhibitor
30 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
GSK2334470 was tested against a panel of 285 kinases and found to be >1,000-fold selective for PDK1, ...

Potency
Cellular
In Vitro

PDPK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm101527u

In Vivo Validations

Mouse
Dose: 100 mg/kg
Route of delivery: Intraperitoneal
Organ of interest (O): xenograft
Target engagement assay: Indirect: inhibition of protein substrate phosphorylation in xenograft tissue

Reference: --

Chemical Information

Molecular Formula C25H34N8O
SMILEs CNc1nc(-c2ccc3c(N)n[nH]c3c2)cc(N2C[C@@H](C(=O)NC3CCCCC3)CC[C@H]2C)n1
InChI InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1
Molecular weight 462.29 Da
AlogP 0.0
HBond acceptors 9
HBond donors 5
Atoms 68

References

Publications

Cross References

canSARChEMBLBindingDB

Expert Reviews

by SERP
(on 21 May 2016 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 8 Sept 2016 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 19 Jun 2017 )
Cellular Use Rating
In Model Organisms
This compound is a potent and selective inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1). It has low nanomolar potency against the PDK1 enzyme. GSK2334470 appears selective based on...
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