Melanocortin receptor 4
A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.
- Measurements
- 20
- Compounds
- 10
- Binding constants
- 7
- Median pX
- —
I · Identity
What this target is
Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.
Melanocortin receptor 4
G protein-coupled receptor that binds melanocyte-stimulating hormones (alpha- and beta-MSH) and corticotropin/ACTH, which are peptide products of the POMC precursor12646665,14764818,25163632,32327598,33858992,8392067. Functions as a central component of the leptin-melanocortin pathway, which is essential for maintaining energy homeostasis32327598,33858992. Upon activation, couples to G(s) protein, stimulating adenylate cyclase and the cAMP-dependent signaling pathway, which promotes anorexogenic signaling in the hypothalamus and contributes to a negative energy balance12588803,14764818,25163632,33858992. Regulates food intake: activation by agonists suppresses appetite, whereas the antagonist Agouti-related protein/AGRP precludes agonist-induced signaling, thereby stimulating appetite9311920,29311635. Modulates the firing activity of neurons in paraventricular nucleus (PVN) of the hypothalamus via alpha-MSH and AGRP regulation of inwardly rectifying potassium channel KCNJ13 closure, independently of G(s) signaling32327598. In the PVN, also interacts with opsin 3/OPN3, which couples to G(i/o) proteins to inhibit MC4R-mediated cAMP signaling, thereby promoting food intake39951488. In intestinal epithelial cells, contributes to inhibition of hepatic glucose production via nesfatin-1/NUCB2, leading to increased cAMP levels and glucagon-like peptide 1 (GLP-1) secretion39562740. Interaction with MGRN1 displaces the G(s) protein, further decreasing MC4R signaling activity19737927. Also activated by gamma-MSH, though with low potency8392067
Quoted from UniProt’s FUNCTION annotation for P32245 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.
What it acts with
STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.
Where it sits in the cell
UniProt, curated Cell membrane · Cell projection, cilium membrane
Expression by cell type
Single cell type RNA, the 2 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Other brain neurons11.6 nCPM
- Retinal bipolar cells6.4 nCPM
Expression by tissue
The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.
- retina3.6 nTPM
- brain3.5 nTPM
- fallopian tube2.9 nTPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Equilibrium binding constants 7
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
Functional readouts 13
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291832 |
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |
| Melanocortin receptor 4 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291832 |
| Melanocortin receptor 4 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291832 |
| Melanocortin receptor 4 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291832 |
| Melanocortin receptor 4 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291832 |
| Melanocortin receptor 4 | Other named receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291832 |
| Melanocortin receptor 4 | Other named receptors | IC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1909167 |