BRD4770

BRD4770 : SAM mimetic inhibitor of EHMT2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe BRD4770 is in the process of SERP review.

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Information

EHMT2

SAM mimetic

up to 10 uM

DOI - 10.1021/cb300139y

Probe Availability:

In Vitro Validations

Uniprot ID: Q96KQ7

Target Class: Epigenetic

Target SubClass: Protein methyltransferase

Potency: IC50

Potency Value: 6300 nM

Potency Assay: In vitro enzyme activity assays on the related compound BRD9539. BRD4770 activity was reported to be lower in vitro, but the authors suggest BRD9539 is the active agent in cells.

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Histone-lysine N-methyltransferase EHMT2, NG36, KM ...

DOI Reference: 10.1021/cb300139y

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency end-point : IC50 PRC2 6.3 uM

Potency assay (off target): Activity assay with related compound BRD9539. No activity was detected against SUV39H1 or DNMT1 up to 40 uM. Partial activity was detected against NSD2 at 40 uM.

Probe Selectivity in Vitro:

No activity was detected against a panel of 16 other epigenetic enzymes or 100 kinases.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

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 with 5 different methyltransferases shows BRD9539 has comparable activity against G9a/EHMT2 and PRC2, no activity against SUV39H1 and DNMT1 and approximately 50% inhibition at 40 uM against NSD2. BRD9539 was also tested against a broader enzyme panel at 5-10 uM, comprised of 16 chromatin-modifying enzymes and 100 kinases, which showed no significant inhibition. However given the relatively weak potency against G9a, cellular effects at 5 uM should be treated with caution and interpreted with sceptism as to whether they are on-target or not.

(last updated: 24 Feb 2026 )