Nidufexor

Partial Agonist of NR1H4

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe Nidufexor is in the process of SERP review.

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Information

NR1H4

Partial Agonist

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q96RI1

Target Class: Transcription factor

Target SubClass: Nuclear Receptor

Potency: EC50

Potency Value: 7 nM

Potency Assay: FXR coactivator interaction assay (57% efficacy)

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

Target aliases:

Bile acid receptor, RIP14, HRR1, FXR, BAR, NR1H4, ...

DOI Reference: 10.1021/acs.jmedchem.9b01621

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

Profiling across a panel of enzymes, ion channels, nuclear receptors, and GPCRs demonstrated the high selectivity of Nidufexor for FXR. No activation of human GPBAR1, as determined by measuring the increase of intracellular cAMP levels, no activation of other nuclear receptors such as AR, ERα, GR, PPARγ, PR, or PXR using a TR-FRET assay (EC50 > 30 μM) and no activation of RXR, LXR, GR, PPARγ, or ERα using a cell-based agonist assay (EC50 > 10 μM).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Good validation data available in cells and in vivo for mice, rats, and dogs. Good selectivity over potential off-targets. Partial FXR agonism in vitro and in a cell based assay for induction of FXR target genes. Pruritus is possible at higher doses

(last updated: 19 Dec 2021 )