TP-238

TP-238 : Inhibitor of CECR2, BPTF

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

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Probe TP-238 is in the process of SERP review.

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Information

CECR2
BPTF

Inhibitor

up to 2 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q9BXF3

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 30 nM

Potency Assay: Alphascreen assay

PDB ID for probe-target interaction (3D structure): 7KDZ, 7BLA

Target aliases:

Chromatin remodeling regulator CECR2, KIAA1740, CE ...

DOI Reference: 10.1039/d0ob00506a

Uniprot ID: Q9BXF3

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 10 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): 7KDZ, 7BLA

Target aliases:

Chromatin remodeling regulator CECR2, KIAA1740, CE ...

DOI Reference: 10.1039/d0ob00506a

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): The closest off-target bromodomain inhibition is BRD9 with IC50 of 1.4 µM. TP-238 has been profiled against the panel of 338 kinases and showed no activity at 1 μM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 2 Jun 2023 )