LXR-623

Partial Agonist of NR1H2, NR1H3

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe LXR-623 is in the process of SERP review.

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Information

NR1H2
NR1H3

Partial Agonist

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Probe Availability:

In Vitro Validations

Uniprot ID: P55055

Target Class: NHR

Target SubClass: NR1 Subfamily

Potency: IC 50

Potency Value: 179 nM

Potency Assay: Radio Labelled binding assay

PDB ID for probe-target interaction (3D structure): not publ.

Structure-activity relationship: yes

Target aliases:

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

DOI Reference: 10.1021/jm800799q

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

PPAR and FXR Gal4 transactivation assays show no agonist effects for PPARα, PPARγ, PPARδ and FXR. Binding Assays: PXR 1.77 uM, RXR >10 uM, GR 1.0 uM, MR no binding, AR2.3 uM, PR >1 uM, ERα No binding, ERβ No binding, TRα No binding, TRβ No binding

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This compound is a partial agonist of LXRa making interpretation of its biology in cells very complex. Partial agonists of nuclear receptors do not make good chemical probes. I do not recommend use of this compound.

(last updated: 10 Nov 2020 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 16 Nov 2020 )