SR9238

SR9238 : Inverse Agonist of NR1H2, NR1H3

Structure

SERP Rating

Probe SR9238 is in the process of SERP review.

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Information

NR1H2
NR1H3

Inverse Agonist

up to 10 uM

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Probe Availability:

In Vitro Validations

Uniprot ID: P55055

Target Class: NHR

Target SubClass: NR1 Subfamily

Potency: IC 50

Potency Value: 214 nM

Potency Assay: Co-Transfection Assay

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

Structure-activity relationship: partial, modelling performed on 3L0E

Target aliases:

Oxysterols receptor LXR-beta, UNR, NER, LXRB, NR1H ...

DOI Reference: 10.1021/cb300541g

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectively inhibits liver LXR over peripheral LXR. Outside target family: No activity in a panel of 20 nuclear receptors using Gal4-NR LBD cell-based cotransfection assay.

Probe Selectivity in Cell:

Nuclear receptor specificity panel illustrating the specificity of SR9238. A Gal4-NR LBD cell-based cotransfection assay was utilized. Data were analyzed by ANOVA followed by Tukey’s post hoc test.

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