Protein / target
Muscarinic acetylcholine receptor M2
Protein at a glance
Biological role
G protein-coupled acetylcholine receptor
Strongest disease association
Asthma
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
Muscarinic receptor for acetylcholine, a neurotransmitter found in the brain, neuromuscular junctions and the autonomic ganglia.
View complete UniProt function annotationHide complete annotation
Muscarinic receptor for acetylcholine, a neurotransmitter found in the brain, neuromuscular junctions and the autonomic ganglia (PubMed:24256733, PubMed:3443095, PubMed:36690613). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (PubMed:36690613). CHRM2 is coupled to G(i)/G(o) (GNAI1 or GNAO1) G proteins and mediates signaling by inhibiting adenylate cyclase activity (PubMed:36690613)
Subcellular location
Domains and Gene Ontology detail (23)Hide
Gene Ontology
- Ccholinergic synapse
- Cclathrin-coated endocytic vesicle membrane
- Cdendrite
- Cmembrane
- Cplasma membrane
- Cpostsynaptic membrane
- Cpresynapse
- Csynapse
- Farrestin family protein binding
- FG protein-coupled acetylcholine receptor activity
- Padenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway
- Padenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Synaptic signalling
- ·Postsynaptic cell membrane
- ·cholinergic synapse
- ·postsynaptic membrane
- ·presynapse
G protein-coupled signalling
- ·G protein-coupled acetylcholine receptor activity
- ·adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway
- ·adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
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.
23 medicines meet Open Targets' target-level approved-medicine definition; the 1 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.
Muscarinic acetylcholine receptor M2 antagonist
Indicated for Urinary Bladder, Overactive, Urinary Incontinence, Urinary Incontinence, Urge
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 CHRM2
Gene-level evidence surfaced through the gene CHRM2 that 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.
View evidence synthesis (4)Hide
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.
Show all associationsHide all associations
Drug development
30 compounds recorded · 23 approved · 6 in clinical development · 1 earlier-stage
View all recorded compounds (10)Hide
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 (9)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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 a drug that targets 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.
- New publicationEfficacy and safety of transdermal and oral oxybutynin in children with neurogenic detrusor overactivity.
- Regulatory approval
Approval: Kentera (previously Oxybutynin Nicobrand) (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.