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Context, anatomy, and key evidence

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MC4R agonist

Setmelanotide

Published evidence · coverage incomplete

Anatomy in the research

Anatomy evidence is still being assembled.

These are anatomical mentions in cited research—not established treatment targets or proof of benefit in people.

This publication has no anatomy passages that meet our source-linking checks yet. Read the available findings ↓

General anatomy view only. No peptide-specific structures are highlighted.

At a glance

What is it—and why does it matter?

Setmelanotide is chemically characterized as an octapeptide with a cyclic structure.

Sources for this introduction: [1]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

Identity

Setmelanotide is chemically characterized as an octapeptide with a cyclic structure.

Sources[2]iuphar-commentsIUPHAR ligand commentaryChemically it is an eight-amino-acid cyclic peptide,
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Chemically it is an eight-amino-acid cyclic peptide,”

    IUPHAR ligand commentary · General comments

    iuphar-comments:9272:94c300d93cf2:94c300d93cf2

How does it work?

Target, response, and disposition.

Mechanism

In a human T-Rex-293 cell cAMP-accumulation assay, setmelanotide acted as an MC1R agonist with sub-nanomolar potency (EC50 0.1585 nM), indicating strong receptor activation in this in vitro system.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL3301624Molecule: CHEMBL3301624 Target: Melanocyte-stimulating hormone receptor (CHEMBL3795) Assay: Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay Assay format: cell-based format Standard result: EC50 = 0.1585 nM pChEMBL value: 9.80 Document: CHEMBL5034014
Reported result
EC50 = 0.1585 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL3301624 Target: Melanocyte-stimulating hormone receptor (CHEMBL3795) Assay: Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay Assay format: cell-based format Standard result: EC50 = 0.1585 nM pChEMBL value: 9.80 Document: CHEMBL5034014”

    ChEMBL activities for CHEMBL3301624 · Activity 24362735

    chembl-activities:chembl3301624:d45cbe9a2800:d45cbe9a2800

Mechanism

In a T-REx-293 cell functional readout of cAMP signaling, setmelanotide acted as an MC3R agonist with EC50 0.1514 nM, consistent with high in vitro potency at MC3R under these assay conditions.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL3301624Molecule: CHEMBL3301624 Target: Melanocortin receptor 3 (CHEMBL4644) Assay: Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay Assay format: cell-based format Standard result: EC50 = 0.1514 nM pChEMBL value: 9.82 Document: CHEMBL5034014
Reported result
EC50 = 0.1514 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL3301624 Target: Melanocortin receptor 3 (CHEMBL4644) Assay: Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay Assay format: cell-based format Standard result: EC50 = 0.1514 nM pChEMBL value: 9.82 Document: CHEMBL5034014”

    ChEMBL activities for CHEMBL3301624 · Activity 24362763

    chembl-activities:chembl3301624:d45cbe9a2800:d45cbe9a2800

What has been studied?

What the evidence says.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Risks and interactions

Risks, organized for scanning.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Products and regulatory status

Same ingredient. Different records.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, contraindication, effect, interaction, regulatory, safety
  • 55 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (40), assurance_score_below_0.72 (13), current_regulatory_source_required (8), extraction_ambiguity (54), high_risk_requires_regulatory_or_two_independent_sources (13), no_direct_support (52)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL3301624 ↗

    chembl-activities · published 2026-08-29 · retrieved 2026-08-29T08:37:13Z

  2. IUPHAR ligand commentary ↗

    iuphar-comments · published 2026-08-29 · retrieved 2026-08-29T08:37:13Z

Publication history and provenance

Version 2 · Automated assessment · 2026-08-29T08:37:13Z

7ac4d960a3c0e19f5b1ef44de40bd7958e5b5d07ec076139ae4ab6b67a5c48d5