BRD4770

BRD4770 : SAM mimetic inhibitor of EHMT2

Structure

SERP Rating

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

No SERP comments found for BRD4770