Protein / target
Melatonin receptor type 1A
Protein at a glance
Biological role
G protein-coupled receptor
Primary biology
GPCR signalling
Strongest disease association
Sleep Initiation and Maintenance Disorders
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
High affinity receptor for melatonin.
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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)
Subcellular location
Domains and Gene Ontology detail (9)Hide
Gene Ontology
- Cplasma membrane
- Creceptor complex
- FG protein-coupled receptor activity
- Fhormone binding
- Fmelatonin receptor activity
- Padenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- Pcircadian rhythm
- PG protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
- Pmating behavior
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Synaptic signalling
- ·High affinity receptor for melatonin. Likely to mediate the reproductive and circadian a…
G protein-coupled signalling
- ·G protein-coupled receptor activity
- ·adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- ·G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messen…
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Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
4 medicines meet Open Targets' target-level approved-medicine definition; the 3 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Melatonin receptor agonist
Indicated for Autistic Disorder, Sleep Initiation and Maintenance Disorders
Melatonin receptor agonist
Indicated for Sleep Disorders, Circadian Rhythm, Sleep Wake Disorders
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene MTNR1A
Gene-level evidence surfaced through the gene MTNR1Athat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
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The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.
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Drug development
5 compounds recorded · 4 approved · 1 in clinical development
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Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
View underlying tractability evidence (8)Hide
Raw Open Targets tractability assessment buckets, by modality.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 3 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Supplemental approval
Supplemental approval: TASIMELTEON (NDA205677)
- Trial status changed
A Multicenter, Double-blind, Randomized Study to Evaluate the Effects of Tasimelteon vs. Placebo in Participants With Delayed Sleep-Wake Phase Disorder (DSWPD)
- Trial status changed
The Effect of Preoperative Oral Melatonin on Postoperative Pain Control After Cesarean Section: A Dose Comparison Study
- New publicationMolecular Links Between Circadian Rhythm Disruption, Melatonin, and Neurodegenerative Diseases: An Updated Review.
- New publicationDysfunctional mitochondria in age-related neurodegeneration: Utility of melatonin as an antioxidant treatment.
- New publicationThe Role of Gut Microbiome in Sleep Quality and Health: Dietary Strategies for Microbiota Support.
- New publicationPresence of melatonin in foods of daily consumption: The benefit of this hormone for health.
- Regulatory approval
Approval: Melatonin Neurim (EMA)
- Regulatory approval
Approval: Hetlioz (EMA)
- Safety communication
Drug Safety Update: Agomelatine (Valdoxan): risk of liver toxicity
- Safety communication
Drug Safety Update: Agomelatine (Valdoxan/ Thymanax): risk of dose-related hepatotoxicity and liver failure
- Regulatory approval
Approval: Circadin (EMA)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.