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OICR-9429 | Antagonist of WDR5
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
WDR5
  • Kd:93 nM
  • IC50:223 nM
Antagonist
500 nM - 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
No activity detected against 9 WDR40 or epigenetic reader proteins.
Selectivity Assessment Description:
No binding or inhibition was detected against 22 protein methyltransferases. Negligible activity ...

Potency
Cellular
In Vitro

WDR5

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1859

Negative Control Compounds

OICR-0547

Chemical Information

Molecular Formula C29H32F3N5O3
SMILEs CN1CCN(c2ccc(-c3cccc(CN4CCOCC4)c3)cc2NC(=O)c2c[nH]c(=O)cc2C(F)(F)F)CC1
InChI InChI=1S/C29H32F3N5O3/c1-35-7-9-37(10-8-35)26-6-5-22(21-4-2-3-20(15-21)19-36-11-13-40-14-12-36)16-25(26)34-28(39)23-18-33-27(38)17-24(23)29(30,31)32/h2-6,15-18H,7-14,19H2,1H3,(H,33,38)(H,34,39)
Molecular weight 555.25 Da
AlogP 3.897
HBond acceptors 8
HBond donors 2
Atoms 72

Vendors

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Expert Reviews

by SERP
(on 17 May 2016)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP
(on 18 May 2016)
Cellular Use Rating
OICR-9429 is a small-molecule antagonist of the WDR5-MLL protein-protein interaction, a notoriously difficult class of molecular targets. There is solid evidence showing a direct in vitro interaction...
by SERP
(on 20 Jun 2016)
Cellular Use Rating
In Model Organisms
...
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