Protein / target
Glycine receptor subunit alpha-1
Protein at a glance
Biological role
Glycine-gated chloride channel activity
Primary system
Nervous system
Strongest disease association
hereditary hyperekplexia
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
6 approved
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Subunit of heteromeric glycine-gated chloride channels (PubMed:14551753, PubMed:23994010, PubMed:25730860, PubMed:37821459). Plays an important role in the down-regulation of neuronal excitability (PubMed:8298642, PubMed:9009272). Contributes to the generation of inhibitory postsynaptic currents (PubMed:25445488). Channel activity is potentiated by ethanol (PubMed:25973519). Potentiation of channel activity by intoxicating levels of ethanol contribute to the sedative effects of ethanol (By similarity)
Subcellular location
Domains and Gene Ontology detail (37)Hide
Gene Ontology
- Cchloride channel complex
- Cdendrite
- Cexternal side of plasma membrane
- Cglycinergic synapse
- Cinhibitory synapse
- Cintracellular membrane-bounded organelle
- Cmembrane
- Cneuron projection
- Cneuronal cell body
- Cperikaryon
- Cplasma membrane
- Cpostsynaptic membrane
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Synaptic signalling
- ·Subunit of heteromeric glycine-gated chloride channels (PubMed:14551753, PubMed:23994010…
- ·Postsynaptic cell membrane
- ·Synapse
- ·glycinergic synapse
Inhibitory neurotransmission
- ·Subunit of heteromeric glycine-gated chloride channels (PubMed:14551753, PubMed:23994010…
- ·glycinergic synapse
- ·inhibitory synapse
- ·inhibitory postsynaptic potential
Chloride transport
- ·Subunit of heteromeric glycine-gated chloride channels (PubMed:14551753, PubMed:23994010…
- ·chloride channel complex
- ·extracellularly glycine-gated chloride channel activity
- ·chloride transport
Ion channel gating
- ·excitatory extracellular ligand-gated monoatomic ion channel activity
- ·ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membr…
- ·transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic…
Ligand-gated signalling
- ·excitatory extracellular ligand-gated monoatomic ion channel activity
- ·ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membr…
- ·transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic…
Muscle contraction
- ·muscle contraction
View underlying pathways (1)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.
Glycine receptor (alpha-1/beta) positive modulator
Appears in clinical studies involving kidney injury, Hydrocephalus, delirium, sedation
Glycine receptor (alpha-1/beta) positive modulator
Appears in clinical studies involving septic shock, Sepsis
Glycine receptor (alpha-1/beta) positive modulator
Appears in clinical studies involving endometrial cancer, myocardial infarction, sedation, delirium
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 2,235 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 · 6 total
kidney injury · Hydrocephalus · delirium
Fever · Pain · Pain
septic shock · Sepsis
Intellectual disability · cognitive disorder · delirium
endometrial cancer · myocardial infarction · sedation
septic shock · Sepsis
Tractability
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 3 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- New publicationNeonatal sevoflurane exposures inhibits DHHC5-mediated palmitoylation of TfR1 in oligodendrocytes, leading to hypomyelination and neurological impairments.
- New publicationEarly exposure to common anesthetic agents causes widespread neurodegeneration in the developing rat brain and persistent learning deficits.
- New publicationSharp wave-associated high-frequency oscillation (200 Hz) in the intact hippocampus: network and intracellular mechanisms.
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.