CRN04894

CRN04894 : Antagonist of MC2R

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe CRN04894 is in the process of SERP review.

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Information

MC2R

Antagonist

up to 100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q01718

Target Class: GPCR

Target SubClass: Adrenocorticotropic hormone receptor

Potency: Ki

Potency Value: 2.1 nM

Potency Assay: Radio ligand binding assay using cell membranes

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

Target aliases:

Adrenocorticotropic hormone receptor, ACTHR, MC2R, ...

DOI Reference: 10.1021/acsmedchemlett.3c00514

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selective against human MC1R MC3R MC4R MC5R with IC50s >10 uM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

As PubChem CID 146361282 this looks a useful probe. Crinetics are also progressing it as a drug, Atumelnant, in two clinical trials https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=clinical&ligandId=13339

(last updated: 13 Aug 2024 )