Selectivity · fingerprint

Agouti (ASIP): receptor selectivity

Agouti (ASIP) blocks MC1R most tightly of the five melanocortin receptors — about 2.5 nM — and prefers it over MC4R by roughly 20×, a selective fingerprint.

By melanocortin.com editorialLast updated 2026
Agouti (ASIP)Endogenous
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the pigment brake

Primary targetMC1Rskin · pigment
Selectivity window20×over MC4R
Selective · blocker
MC1Rskin · pigment
8.6ᵐblocks · ≈2.5 nMprimary
MC2Radrenal · cortisol
no curated value
MC3Renergy balance
6.7ᵐblocks · ≈200 nM
MC4Rappetite · satiety
7.3ᵐblocks · ≈50 nM
MC5Rexocrine glands
4.9ᵐblocks · ≈13 µM

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

A genuine single-receptor lean — one of the few melanocortins that is not broadly promiscuous.

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 Agouti (ASIP) 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.