dBRD9

Degrader (PROTAC) of BRD9

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

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Information

BRD9

Degrader (PROTAC)

100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9H8M2

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 104 nM

Potency Assay: AlphaScreen

PDB ID for probe-target interaction (3D structure): 5TWX

Structure-activity relationship: yes

Target aliases:

Bromodomain-containing protein 9, BRD9, BRD9_HUMAN ...

DOI Reference: 10.1002/anie.201611281

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

BromoScan @ 1uM BRD4 > 50 uM, no off-targets. on detectable degradation of off-targets by western blot. Outside target family: Proteomic Mass Spectrometry shows that BRD9 is the only protein degraded of 7326 quantified. Degrades the IKZF family of linage specific transcription factors.

Potency assay, off target (cells): western blot

Probe Selectivity in Cell:

no detectable degradation of off-targets

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(last updated: 19 Jan 2021 )

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(last updated: 9 Feb 2021 )

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(last updated: 18 Feb 2021 )