Apelin receptor
A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.
- Measurements
- 7
- Compounds
- 2
- Binding constants
- 0
- 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.
Apelin receptor
G protein-coupled receptor for peptide hormones apelin (APLN) and apelin receptor early endogenous ligand (APELA/ELA), that plays a role in the regulation of normal cardiovascular function and fluid homeostasis11090199,22810587,25639753,28137936,35817871,38428423. When acting as apelin receptor, activates both G(i) protein pathway that inhibits adenylate cyclase activity, and the beta-arrestin pathway that promotes internalization of the receptor11090199,25639753,28137936,35817871,38428423. APLNR/APJ also functions as mechanoreceptor that is activated by pathological stimuli in a G protein-independent fashion to induce beta-arrestin signaling, hence eliciting cardiac hypertrophy22810587,38428423. However, the presence of apelin ligand blunts cardiac hypertrophic induction from APLNR/APJ on response to pathological stimuli22810587,38428423. Plays a key role in early development such as gastrulation, blood vessels formation and heart morphogenesis by acting as a APELA receptor (By similarity). May promote angioblast migration toward the embryonic midline, i.e. the position of the future vessel formation, during vasculogenesis (By similarity). Promotes sinus venosus (SV)-derived endothelial cells migration into the developing heart to promote coronary blood vessel development (By similarity). Also plays a role in various processes in adults such as regulation of blood vessel formation, blood pressure, heart contractility and heart failure25639753,28137936
(Microbial infection) Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia11090199
Quoted from UniProt’s FUNCTION annotation for P35414 (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
Expression by cell type
Single cell type RNA, the 3 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.
- Vascular endothelial cells46.8 nCPM
- Astrocytes21.7 nCPM
- Lymphatic endothelial cells19.5 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.
- lymphoid tissue101.5 nTPM
- placenta87.2 nTPM
- brain77.5 nTPM
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Other measurements 7
Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| Apelin receptor | Other named receptors | %Max (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209814 |
| Apelin receptor | Other named receptors | %Inhib (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209814 |
| Apelin receptor | Other named receptors | %Inhib (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209814 |
| Apelin receptor | Other named receptors | %Max (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209814 |
| Apelin receptor | Other named receptors | %Inhib (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209814 |
| Apelin receptor | Other named receptors | %Inhib (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209815 |
| Apelin receptor | Other named receptors | %Inhib (Mean) | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5209816 |