BI-653048

BI 653048 : Agonist of NR3C1

Structure

SERP Rating

In Cells

(2 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 BI-653048 is in the process of SERP review.

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Information

NR3C1

Agonist

1 uM
Reviewer recommended concentration: 2 µM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P04150

Target Class: NHR

Target SubClass: Subfamily 3

Potency: IC50

Potency Value: 55 nM

Potency Assay: Fluorescence polarization assay

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

Target aliases:

, Glucocorticoid receptor, GRL, NR3C1, GCR_HUMAN, ...

DOI Reference: 10.1021/ml500387y

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: > 100 fold selectivity against related nuclear receptors (PGR, NR3C2, ESR1, AR). Selectivity outside target family: 49 Eurofins-Panlabs targets at 10 µM – no hits; Clean GPCR scan.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Consider that BI 653048 has a preference for transrepression over transcriptional activation of GR and therefore only activates some mechanisms of GR activity fully (see 10.1021/ml500387y). BI 653048 should be used in combination with other GR agonists.

(last updated: 22 Feb 2022 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Target binding and in cellular target engagement are well demonstrated. The users should be aware that compound BI-653048 favors transrepression over transactivation and does not cover all GR-activities equally. Selectivity profiling within the family does only cover the most closely related receptors. Cellular profiling was mostly performed at 2 µM.

(last updated: 17 Jun 2024 )