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GSK484 | Mixed-mode inhibitor of PADI4
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 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
PADI4
  • IC50:50 nM
  • IC50:250 nM
Mixed-mode inhibitor
Up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki, Kii - PADI1: Ki = 108 uM, Kii = 470 uM, PADI2 Ki = 107 uM, Kii = 1350 uM, PADI3 Ki = 2090 uM, Kii = 1230 uM, PADI4 Ki = 6.8 uM, Kii = 65 uM

Selectivity Assessment Description:
Negligible activity in a panel of 50 protein kinases Negligible activity against COX2, MAOB, PDE4 ...

Potency
Cellular
In Vitro

PADI4

Mode of Action: Mixed-mode inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.1735

Negative Control Compounds

GSK106

Chemical Information

Molecular Formula C27H31N5O3
SMILEs COc1cc(C(=O)N2CC[C@@H](O)[C@@H](N)C2)cc2nc(-c3cc4ccccc4n3CC3CC3)n(C)c12
InChI InChI=1S/C27H31N5O3/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16/h3-6,11-13,16,19,23,33H,7-10,14-15,28H2,1-2H3/t19-,23+/m0/s1
Molecular weight 473.24 Da
AlogP 3.147700000000002
HBond acceptors 8
HBond donors 3
Atoms 66

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 18 May 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 20 Dec 2016 )
Cellular Use Rating
In Model Organisms
GSK484 is a PADI4-selective in vitro chemical probe. PAD4 is a calcium-dependent enzyme which catalyzes the reaction in which protein arginine residues are converted into citrulline, with the release...
by SERP
(on 7 Jul 2017 )
Cellular Use Rating
In Model Organisms
There is solid experimental evidence supporting GSK484 as a PAD4-specific inhibitor in biochemical systems, including nanomolar potencies in fluorescence polarization, ligand-competition, and NH3-release...

Portal Comments

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(last updated: 7 Nov 2023)

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