Vimirogant

Inhibitor of RORC

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe Vimirogant is in the process of SERP review.

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Information

RORC

Inhibitor

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Probe Availability:

In Vitro Validations

Uniprot ID: P51449

Target Class: Transcription factor

Target SubClass: NR1 nuclear hormone receptors

Potency: IC50

Potency Value: 3.7 nM

Potency Assay: radio-ligand RORγ binding scintillation proximity assay

PDB ID for probe-target interaction (3D structure): 5NTW

Structure-activity relationship: yes

Target aliases:

Nuclear receptor ROR-gamma, RZRG, RORG, NR1F3, ROR ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

more than 1000-fold selectivity against other ROR isoforms

Probe Selectivity in Cell:

inhibit hERG by 45.4% at 3 μM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Vimirogant is a RORgt inverse agonist with potent cellular activity and more than 1000-fold selectivity over RORa and RORb. It has been dosed orally in man in phase I and phase II clinical studies. Limited preclinical species PK data is publicly available but indications are that Vimirogant can be dosed up to 100mg/kg in mice.

(last updated: 21 Jun 2021 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This compound is an inhibitor of RORc, that was developed as a therapeutic for autoimmune diseases by Vitae Pharmaceuticals (now Allergan Pharmaceutical). The compound is reported to induce the expression of IL-17 in human whole blood at a concentration above 200 nM. Evidence suggests that psoriasis patients showed improvements after treatment suggesting the compound could be working in vivo. The data provided in the DOI is a summary from patent applications made by the company and hasn’t been peer-reviewed. There is no reason to believe the compound is not efficiently inhibiting RORc, however, the correct concentrations for your experiments should be determined through experimentation.

(last updated: 7 Jul 2021 )