GSK8814

Inhibitor of ATAD2, ATAD2B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe GSK8814 is in the process of SERP review.

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Information

ATAD2
ATAD2B

Inhibitor

up to 10 uM

Additional Data

SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: Q6PL18

Target Class: Epigenetic

Target SubClass: ATPase

Potency: Kd

Potency Value: 7.94 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): 5LJ0

Structure-activity relationship: yes

Target aliases:

ATPase family AAA domain-containing protein 2, ATA ...

DOI Reference: 10.1002/anie.201603928

Uniprot ID: Q6PL18

Target Class: Epigenetic

Target SubClass: ATPase

Potency: Ki

Potency Value: 1.25 nM

Potency Assay: BROMOscan

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

Target aliases:

ATPase family AAA domain-containing protein 2, ATA ...

DOI Reference: 10.1002/anie.201603928

Uniprot ID: Q6PL18

Target Class: Epigenetic

Target SubClass: ATPase

Potency: IC 50

Potency Value: 50.1 nM

Potency Assay: TR-FRET

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

Target aliases:

ATPase family AAA domain-containing protein 2, ATA ...

DOI Reference: 10.1002/anie.201603928

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): BROMOscan

Probe Selectivity in Vitro:

GSK8814 is more than 100 folds selective over all other bromodomains in the BROMOscan. More than 1000 folds selective over BRD4.

Outside Target Family: GSK8814 was inactive against an internal GSK panel of 40 targets considered as potential liabilities.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

No in Vitro data is available at this time. More data needed and need more update

(last updated: 4 Jan 2022 )