ELAGOLIX

ELAGOLIX : Antagonist of GNRHR

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe ELAGOLIX is in the process of SERP review.

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Information

GNRHR

Antagonist

up to 100 nM

In Vitro Validations

Uniprot ID: P30968

Target Class: GPCR

Target SubClass: GnRH receptor

Potency: Ki

Potency Value: 0.9 nM

Potency Assay: Competition binding assay

PDB ID for probe-target interaction (3D structure): 7BR3

Target aliases:

Gonadotropin-releasing hormone receptor, GRHR, GNR ...

DOI Reference: 10.1021/jm8006454

Uniprot ID: P30968

Target Class: GPCR

Target SubClass: GnRH receptor

Potency: Kd

Potency Value: 0.54 nM

Potency Assay: Radiolingand binding assay

PDB ID for probe-target interaction (3D structure): 7BR3

Target aliases:

Gonadotropin-releasing hormone receptor, GRHR, GNR ...

DOI Reference: 10.1021/jm8006454

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Elagolix was highly selective at hGnRH-R, its wider receptor selectivity was tested at a concentration of 10 μM in a panel of radioligand binding assays for 100 off-target receptors, ion channels, enzymes, and transporters, and significant activity was not observed (inhibition <50%).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Elagolix is a clinically validated GnRHR antagonist with strong utility as a chemical probe in systems where human GnRH receptor is expressed and functionally relevant. Elagolix is a highly effective tool for target validation, pharmacological studies, and in vivo hormone suppression. It is best used with careful consideration of species differences, off-target risks, and downstream hormonal effects. Having a structural analogue of Elagolix that is inactive as a negative probe would be very useful in pharmacological studies (see reference DOI: 10.1021/acs.jmedchem.6b01071 for some possible hGnRHR negative probes)

(last updated: 16 May 2025 )