Selectivity · fingerprint

Setmelanotide: receptor selectivity

Setmelanotide binds MC4R most tightly of the five melanocortin receptors — about 2.0 nM — and prefers it over MC1R by roughly 2.0×, a broadly non-selective fingerprint.

By melanocortin.com editorialLast updated 2026
SetmelanotideApproved drug
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MC4R drug, broad binder

Primary targetMC4Rappetite · satiety
Selectivity window2.0×over MC1R
Broadly non-selective
MC1Rskin · pigment
8.4≈4.0 nM
MC2Radrenal · cortisol
no curated value
MC3Renergy balance
8.0≈10 nM
MC4Rappetite · satiety
8.7≈2.0 nMprimary
MC5Rexocrine glands
6.4≈398 nM

Bars are sized by binding strength (p-value, on a fixed MC1R–MC5R scale);ᵐ marks a mouse value.

Effectively non-selective: Setmelanotide grips several receptors within an order of magnitude of each other, so it is not a clean single-target molecule.

The selectivity window is the fold-gap between a ligand's tightest and second-tightest receptor — a compact measure of how cleanly it picks a target. One caveat it cannot capture: binding is not function. These bars show how tightly Setmelanotide holds each receptor, not what the receptor then does downstream. To put this ligand next to the others, use the selectivity visualizer; for every value with its citation, the binding matrix.

Affinity values from the IUPHAR/BPS Guide to PHARMACOLOGY; the selectivity window is derived from them. Educational resource, not medical advice — see the editorial standards.