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ARUK2002821 | ARUK2002821 : Inhibitor of PIP4K2A
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
PIP4K2A
  • IC50:10 nM
  • IC50:250 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective against isoforms PI5P4Kγ(IC50 >39 uM) and PI5P4Kβ (IC50 ND). ARUK2002821 was profiled aga ...

Potency
Cellular
In Vitro

PIP4K2A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1039/D3MD00039G

Chemical Information

Molecular Formula C21H19ClN4O
SMILEs COc1ccc(Nc2ncnc3c2ccn3-c2ccc(C)c(C)c2)cc1Cl
InChI InChI=1S/C21H19ClN4O/c1-13-4-6-16(10-14(13)2)26-9-8-17-20(23-12-24-21(17)26)25-15-5-7-19(27-3)18(22)11-15/h4-12H,1-3H3,(H,23,24,25)
Molecular weight 378.12 Da
AlogP 0.0
HBond acceptors 5
HBond donors 1
Atoms 46
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

canSARChEMBLPDB

Expert Reviews

by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
The compound has been profiled against a panel of around 155 kinases and demonstrated good selectivity. No screened kinase showed >50% inhibition at 1μm, except the target PIP5K2a(PI5P4Ka) showing 85%...
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