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GSK481 | Inhibitor of RIPK1
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
RIPK1
  • Ki:0.8 nM
  • IC50:10 nM
Inhibitor
10-100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
GSK481 was tested at 10 μM in duplicate against 318 kinases in the Reaction Biology Corporation (RBC ...

Potency
Cellular
In Vitro

RIPK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.5b01898

Negative Control Compounds

5-benzyl-N-[(3R)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1,2-oxazole-3-carboxamide

Orthogonal Probes def

GSK2982772

Chemical Information

Molecular Formula C21H19N3O4
SMILEs CN1C(=O)[C@@H](NC(=O)c2cc(Cc3ccccc3)on2)COc2ccccc21
InChI InChI=1S/C21H19N3O4/c1-24-18-9-5-6-10-19(18)27-13-17(21(24)26)22-20(25)16-12-15(28-23-16)11-14-7-3-2-4-8-14/h2-10,12,17H,11,13H2,1H3,(H,22,25)/t17-/m0/s1
Molecular weight 377.14 Da
AlogP 2.4192
HBond acceptors 7
HBond donors 1
Atoms 47

References

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Expert Reviews

by SERP
(on 9 Mar 2017 )
Cellular Use Rating
GSK481 is a remarkably potent and selective inhibitor of RIPK1 that is suitable to interrogate this target in cells. On the other hand, it may not be suitable for in vivo use, as RIPK1 orthologs show...
by SERP
(on 17 Mar 2017 )
Cellular Use Rating
Despite being highly selective and potent, GSK481 should only be used as chemical probe in cells.
by SERP
(on 21 Mar 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
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