Protein / target
Glutamate receptor ionotropic, kainate 3
Protein at a glance
Biological role
Kainate selective glutamate receptor
Strongest disease association
Major depressive disorder
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
Ionotropic glutamate receptor that functions as a cation-permeable ligand-gated ion channel, gated by L-glutamate and the glutamatergic agonist kainic acid.
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Ionotropic glutamate receptor that functions as a cation-permeable ligand-gated ion channel, gated by L-glutamate and the glutamatergic agonist kainic acid. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist (PubMed:7719709). In association with GRIK2, involved in presynaptic facilitation of glutamate release at hippocampal mossy fiber synapses (By similarity)
Subcellular location
Domains and Gene Ontology detail (23)Hide
Gene Ontology
- Caxon
- Cdendrite
- Cdendrite cytoplasm
- Cglutamatergic synapse
- Ckainate selective glutamate receptor complex
- Cperikaryon
- Cplasma membrane
- Cpostsynaptic density membrane
- Cpresynaptic membrane
- Cterminal bouton
- Fadenylate cyclase inhibiting G protein-coupled glutamate receptor activity
- Fglutamate receptor activity
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Excitatory neurotransmission
- ·Ionotropic glutamate receptor that functions as a cation-permeable ligand-gated ion chan…
- ·glutamatergic synapse
- ·negative regulation of synaptic transmission, glutamatergic
- ·synaptic transmission, glutamatergic
Ligand-gated signalling
- ·Ionotropic glutamate receptor that functions as a cation-permeable ligand-gated ion chan…
- ·ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membr…
- ·transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic…
Ion channel gating
- ·glutamate-gated calcium 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…
G protein-coupled signalling
- ·adenylate cyclase inhibiting G protein-coupled glutamate receptor activity
- ·G protein-coupled glutamate 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.
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.
Glutamate receptor ionotropic kainate antagonist
Indicated for Epilepsy, Migraine Disorders, Seizures
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 GRIK3
Gene-level evidence surfaced through the gene GRIK3 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.
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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
4 compounds recorded · 1 approved · 3 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.
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.
- Regulatory approval
Approval: TOPIRAMATE (ANDA219183)
- Product recall
Recall (Class III): TOPIRAMATE
- Regulatory approval
Approval: TOPIRAMATE (ANDA220943)
- Product recall
Recall (Class III): TOPIRAMATE
- Supplemental approval
Supplemental approval: PHENTERMINE AND TOPIRAMATE (NDA022580)
- Label change
Label change: TOPIRAMATE (ANDA078499)
- Safety communication
Drug Safety Update: Topiramate (Topamax): introduction of new safety measures, including a Pregnancy Prevention Programme
- Safety communication
Drug Safety Update: Topiramate (Topamax): start of safety review triggered by a study reporting an increased risk of neurodevelopmental disabilities in children with prenatal exposure
- New publicationA randomized pilot trial of topiramate for alcohol use disorder in veterans with traumatic brain injury: Effects on alcohol use, cognition, and post-concussive symptoms.
- New publicationCognitive and behavioral effects of lamotrigine and topiramate in healthy volunteers.
- New publicationA double-blind, randomized trial of topiramate in Lennox-Gastaut syndrome. Topiramate YL Study Group.
- New publicationA randomized, placebo-controlled study of topiramate in primary generalized tonic-clonic seizures. Topiramate YTC Study Group.
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.