Protein / target
Adenosine receptor A1
Protein at a glance
Biological role
G protein-coupled adenosine receptor activity
Primary system
Nervous system
Strongest disease association
asthma
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
7 approved · 15 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Receptor for adenosine (PubMed:29925945). The activity of this receptor is mediated by G proteins such as GNAI2 which inhibit adenylyl cyclase
Subcellular location
Domains and Gene Ontology detail (67)Hide
Gene Ontology
- Casymmetric synapse
- Caxolemma
- Cbasolateral plasma membrane
- Ccalyx of Held
- Cdendrite
- Cdendritic spine
- Cintracellular protein-containing complex
- Cneuronal cell body
- Cplasma membrane
- Cpostsynaptic membrane
- Cpresynaptic active zone
- Cpresynaptic membrane
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
- ·asymmetric synapse
- ·postsynaptic membrane
- ·presynaptic active zone
- ·presynaptic membrane
G protein-coupled signalling
- ·G protein-coupled adenosine receptor activity
- ·G protein-coupled receptor binding
- ·adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- ·G protein-coupled purinergic nucleotide receptor signaling pathway
Excitatory neurotransmission
- ·excitatory postsynaptic potential
- ·negative regulation of synaptic transmission, glutamatergic
Kinase signalling
- ·positive regulation of dephosphorylation
- ·positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
Immune signalling
- ·inflammatory response
- ·negative regulation of acute inflammatory response
Inhibitory neurotransmission
- ·negative regulation of synaptic transmission, GABAergic
View underlying pathways (2)Hide underlying pathways
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.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Adenosine receptor agonist
Appears in clinical studies involving paroxysmal tachycardia, Wolff-Parkinson-White syndrome, cardiovascular disorder, Paroxysmal supraventricular tachycardia
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 636 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 22 total
postherpetic neuralgia · neuropathic pain
paroxysmal tachycardia · Wolff-Parkinson-White syndrome · cardiovascular disorder
migraine disorder · Apnea · Pain
neuropathic pain · peripheral nerve injury
atrial fibrillation · angina pectoris
heart failure · congestive heart failure
familial hyperlipidemia
airway hyperresponsiveness · asthma · atopic asthma
Renal insufficiency · heart failure
Recurrent thrombophlebitis · hepatic veno-occlusive disease · diabetic kidney disease
Tractability
Safety liabilities
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.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
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 underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.
- New publicationAdenosine Receptors in Neuroinflammation and Neurodegeneration.
- New publicationREDIportal: toward an integrated view of the A-to-I editing.
- New publicationAdvances in A-to-I RNA editing in cancer.
- New publicationMicroglia regulate motor neuron plasticity via reciprocal fractalkine and adenosine signaling.
- New publicationAstrocytic neuroligin 3 regulates social memory and synaptic plasticity through adenosine signaling in male mice.
- New publicationWTAP participates in neuronal damage by protein translation of NLRP3 in an m6A-YTHDF1-dependent manner after traumatic brain injury.
- New publicationAdenosine and adenosine receptors in metabolic imbalance-related neurological issues.
- New publicationAstrocytic ALKBH5 in stress response contributes to depressive-like behaviors in mice.
- New publicationAdenosine and Cortical Plasticity.
- New publicationProgrammable RNA N<sup>6</sup>-methyladenosine editing with CRISPR/dCas13a in plants.
- New publicationm<sup>1</sup>A in CAG repeat RNA binds to TDP-43 and induces neurodegeneration.
- New publicationUtilizing AAV-mediated LEAPER 2.0 for programmable RNA editing in non-human primates and nonsense mutation correction in humanized Hurler syndrome mice.
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.