Skip to content
PsychedeliaDokholyan Laboratory
TargetOther named receptors

Melatonin receptor type 1A

A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.

Measurements
3
Compounds
1
Binding constants
1
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.

Protein

MTR1A_HUMANMTNR1AHomo sapiens

Melatonin receptor type 1A

High affinity receptor for melatonin. Likely to mediate the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity. Possibly involved in sleep induction, by melatonin activation of the potassium channel KCNMA1/BK and the dissociation of G-beta and G-gamma subunits, thereby decreasing synaptic transmission (By similarity)

Quoted from UniProt’s FUNCTION annotation for P48039 (reviewed).

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.

PartnerCombinedExperimentDatabaseText mining
GNB10.9800.9350.6500.193
GNAI10.9760.9260.6500.163
GPR500.9550.2920.9000.416
MTNR1B0.9450.2920.9000.276
GNG20.9400.8270.6500.091
FAT10.8710.0000.0000.871
GNAI20.8370.5230.6500.105
GNAI30.8310.5230.6500.072
FAT30.8040.0000.0000.804
GNB40.7840.3890.6500.072

Where it sits in the cell

UniProt, curated Cell membrane

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.

  • kidney1.7 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 0.1 nTPM, from MTNR1Acerebellum — 0.6 nTPM, from MTNR1Ahippocampal formation — no resolved target expressed hereamygdala — no resolved target expressed herehypothalamus — no resolved target expressed herethalamus — no resolved target expressed herebasal ganglia — no resolved target expressed heremedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: retina 0.2.

Body

heart — no resolved target expressed heresmooth muscle — no resolved target expressed herelung — no resolved target expressed hereliver — no resolved target expressed herekidney — 1.7 nTPM, from MTNR1Astomach — 0.1 nTPM, from MTNR1Aduodenum — 0.2 nTPM, from MTNR1Asmall intestine — 0.2 nTPM, from MTNR1Acolon — 0.9 nTPM, from MTNR1Aadrenal gland — no resolved target expressed herethyroid gland — no resolved target expressed herepancreas — 0.8 nTPM, from MTNR1Aurinary bladder — 0.1 nTPM, from MTNR1Askeletal muscle — 0.1 nTPM, from MTNR1Aspleen — no resolved target expressed heresalivary gland — 0.1 nTPM, from MTNR1A
02 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of MTNR1A transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 3

  • cerebellum0.6 nTPM
  • retina0.2 nTPM
  • cerebral cortex0.1 nTPM

Peripheral and autonomic · 9

  • kidney1.7 nTPM
  • colon0.9 nTPM
  • pancreas0.8 nTPM
  • duodenum0.2 nTPM
  • small intestine0.2 nTPM
  • stomach 10.1 nTPM
  • urinary bladder0.1 nTPM
  • skeletal muscle0.1 nTPM
  • salivary gland0.1 nTPM

Transcript is not protein. These are RNA levels for MTNR1A, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 1

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Melatonin receptor type 1AOther named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3583713

Functional readouts 1

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Melatonin receptor type 1AOther named receptorsEC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL3583716

Other measurements 1

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.

TargetClassTypeValue (nM)pXOrganismAssay
Melatonin receptor type 1AOther named receptorsEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL3583717
← All targets