MK-3697

MK-3697 : Antagonist of HCRTR2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe MK-3697 is in the process of SERP review.

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Information

HCRTR2

Antagonist

up to 1 uM
Reviewer recommended concentration: 100 nM due to potential off-target effects

Probe Availability:

In Vitro Validations

Uniprot ID: O43614

Target Class: GPCR

Target SubClass: Orexin receptor

Potency: Ki

Potency Value: 1.1 nM

Potency Assay: Radioligand Binding Assay

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

Target aliases:

Orexin receptor type 2, HCRTR2, OX2R_HUMAN, Ox2R, ...

DOI Reference: 10.1016/j.bmcl.2014.08.041

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selective again OX1 both in vitro and in cells (Ki = 31 µM and IC50 > 10 µM, respectively)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 4 Jan 2024 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

MK-3697 is a good chemical probe/antagonist for hypocretin (orexin) receptor 2 for cellular and in-vivo use. The recommended dose, however, should be lower than 1µM because of potential off-target effects. We recommend a dose of 100nM in cells. It would have been preferable to know the identity of off-target selectivity panel.

(last updated: 14 Oct 2025 )