PF-03882845

PF-03882845 : Antagonist of NR3C2

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe PF-03882845 is in the process of SERP review.

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Information

NR3C2

Antagonist

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P08235

Target Class: NHR

Target SubClass: Mineralocorticoid receptor

Potency: IC50

Potency Value: 0.755 nM

Potency Assay: serum-free functional reporter assay utilizing the human MR ligand-binding domain

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

Target aliases:

Mineralocorticoid receptor, MLR, MCR, NR3C2, MCR_H ...

DOI Reference: 10.3389/fphar.2013.00115

Uniprot ID: P08235

Target Class: NHR

Target SubClass: Mineralocorticoid receptor

Potency: IC50

Potency Value: 2.7 nM

Potency Assay: Radioligand binding assay

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

Target aliases:

Mineralocorticoid receptor, MLR, MCR, NR3C2, MCR_H ...

DOI Reference: 10.1021/jm100505n

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity factor of 115-fold for MR over PR (IC50=310 nM). Tested for PR agonist activity and were found to be inactive up to concentrations of 100 μM. Selective against AR (>8910 nM), ERalpha (>10000 nM), GR (>10000nM) and PR (416 nM).

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In Cell Rating

In Model Organisms

(last updated: 13 Jun 2022 )