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BRD4770 | BRD4770 : SAM mimetic inhibitor of EHMT2
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
EHMT2
  • IC50:6300 nM
  • EC50:5000 nM
SAM mimetic
up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PRC2 6.3 uM

Potency Assay Off-Target:
Activity assay with related compound BRD9539. No activity was detected against SUV39H1 or DNMT1 up t ...
Selectivity Assessment Description:
No activity was detected against a panel of 16 other epigenetic enzymes or 100 kinases.

Potency
Cellular
In Vitro

EHMT2

Mode of Action: SAM mimetic

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/cb300139y

Chemical Information

Molecular Formula C25H23N3O3
SMILEs COC(=O)c1ccc2c(c1)nc(NC(=O)c1ccccc1)n2CCCc1ccccc1
InChI InChI=1S/C25H23N3O3/c1-31-24(30)20-14-15-22-21(17-20)26-25(27-23(29)19-12-6-3-7-13-19)28(22)16-8-11-18-9-4-2-5-10-18/h2-7,9-10,12-15,17H,8,11,16H2,1H3,(H,26,27,29)
Molecular weight 413.17 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 54

References

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Cross References

canSARChEMBLBindingDB

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Expert Reviews

by SERP
(on 24 Feb 2026)
Cellular Use Rating
BRD4770, although not active in biochemical assays itself against G9a, is thought to be a methyl ester pro-drug of the biochemically active compound BRD9539 (biochemical G9a IC50 = 6.3 uM). In vitro assays...
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