BI-7190

BI-7190 : Inhibitor of BPTF

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe BI-7190 is in the process of SERP review.

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Information

BPTF

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q12830

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 3.5 ± 2.8 nM

Potency Assay: DiscoveRx

PDB ID for probe-target interaction (3D structure): 8AG2

Target aliases:

Nucleosome-remodeling factor subunit BPTF, FALZ, F ...

DOI Reference: 10.1002/cmdc.202200686

Uniprot ID: Q12830

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 131 ± 24 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): 8AG2

Target aliases:

Nucleosome-remodeling factor subunit BPTF, FALZ, F ...

DOI Reference: 10.1002/cmdc.202200686

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): No significant hits were observed in Kinase and CEREP panel. BI-7190 shows high selectivity at 10 µM concentration versus a panel of 44 receptors (no inhibition), Kinase panel (38 kinases, no hit at 10 µM). The negative control BI-4827 shows high selectivity hitting 0/44 targets inhibition with more than 50% @10 µM.

Potency assay, off target (cells): NanoBRET EC50 BRD9 1100 nM, BRPF1 2960 nM, CECR2 13200 nM

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

BI-7190 is a selective, high-affinity chemical probe that targets the bromodomain of the transcription factor BPTF. This compound demonstrates high in vitro affinity for BPTF in two different biochemical assays, as well as great intracellular target engagement in a NanoBRET assay at low nanomolar concentrations. Importantly, BI-7190 also has limited off-target activity with other bromodomains and kinases, as indicated by kinase profiling and SafetyScreen44 assay results, thus confirming its cellular selectivity. These results validate the utility of BI-7190 as an excellent chemical tool for studying BPTF target engagement across different cellular contexts, thus providing better mechanistic insight into the function of BPTF in these cells.

(last updated: 30 May 2025 )