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Protein / target

Transient receptor potential cation channel subfamily V member 1

Encoded byTRPV1Q8NER1Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
3
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Extracellular ligand-gated monoatomic ion channel

Strongest disease association

Migraine Disorders

Via encoding gene TRPV1 · Clinical evidence · score 0.63

Therapeutic position

Established drug target

Small molecules

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli.

View complete UniProt function annotation

Non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli (PubMed:11050376, PubMed:11243859, PubMed:11226139, PubMed:12077606). Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Activated by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius (PubMed:37117175). Upon activation, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis

Subcellular location

Postsynaptic cell membraneCell projection, dendritic spine membraneCell membrane
Domains and Gene Ontology detail (30)

Gene Ontology

  • Cdendritic spine membrane
  • CGABA-ergic synapse
  • Cmembrane
  • Cplasma membrane
  • Cpostsynaptic membrane
  • FATP binding
  • Fcalcium channel activity
  • Fcalmodulin binding
  • Fexcitatory extracellular ligand-gated monoatomic ion channel activity
  • Fextracellular ligand-gated monoatomic ion channel activity
  • Fintracellularly gated calcium channel activity
  • Fmetal ion binding

839 aa · 95 kDa · 2 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Ion channel gatingGOLigand-gated signallingGOReceptor tyrosine kinase signallingUniProt
View supporting evidence

Ion channel gating

  • ·excitatory extracellular ligand-gated monoatomic ion channel activity
  • ·extracellular ligand-gated monoatomic ion channel activity
  • ·temperature-gated ion channel activity
  • ·calcium ion transmembrane transport

Ligand-gated signalling

  • ·excitatory extracellular ligand-gated monoatomic ion channel activity
  • ·extracellular ligand-gated monoatomic ion channel activity
  • ·temperature-gated ion channel activity

Receptor tyrosine kinase signalling

  • ·Non-selective calcium permeant cation channel involved in detection of noxious chemical…
View underlying pathways (1)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

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.

CALM3TRPM8CALML3CALML5TRPA1CALML4CALML6PRKACBPRKACAPRKACGTRPV1

10 strongest partners — larger node and heavier line mean higher confidence

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

2 medicines · 12 areas

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.

Arthritis2 medicines
Back Pain2 medicines
Pain2 medicines
Acute Pain1 medicine
Common Cold1 medicine
Contusions1 medicine
Fever1 medicine
Headache1 medicine
Influenza, Human1 medicine
Migraine Disorders1 medicine
Neuralgia1 medicine
Osteoarthritis1 medicine

3 medicines meet Open Targets' target-level approved-medicine definition; the 2 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

2

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.

Capsaicin
Narrow target profileApprovedOpener

Vanilloid receptor opener

Indicated for Arthritis, Back Pain, Contusions, Neuralgia

Direct interaction with this protein · Only this protein recorded as a target

acetaminophen
ApprovedOpener

Vanilloid receptor opener

Indicated for Acute Pain, Arthritis, Back Pain, Common Cold

Direct interaction with this protein · 1 of 4 recorded protein targets

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

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 TRPV1

Gene-level evidence surfaced through the gene TRPV1 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.

Migraine Disorders
0.78Well supported

Clinical evidence dominant · Open Targets 0.63

Arthritis
0.75Well supported

Clinical evidence dominant · Open Targets 0.61

View evidence synthesis (2)
Migraine DisordersWell supported
0.78
agreement 0.620.93
Clinical86%Literature14%

Open Targets aggregate 0.63 · 2 independent evidence families

ArthritisWell supported
0.75
agreement 0.600.91
Clinical89%Literature11%

Open Targets aggregate 0.61 · 2 independent evidence families

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 associations
Migraine Disorders0.63
Arthritis0.61

Drug development

19 compounds recorded · 3 approved · 16 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 2 drugs that target this protein in Forefront's canonical graph (2 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
ABT-102Phase 1
ZUCAPSAICINApproval
MAVATREPPhase 1
SB-705498Phase 2
PAC-14028Phase 3
AZD1386Phase 2
ACETAMINOPHENApproval
SAF312Phase 2
PHE377Phase 1
DWP05195Phase 2

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 moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Advanced Clinical support this modality.

View underlying tractability evidence (10)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Small Molecule BinderOC · Advanced Clinical

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

neurotoxicityClinPGx

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

30

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)

ENROLLING_BY_INVITATION · via acetaminophen · NCT06997016

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 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.

  1. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE (ANDA040779)

    fda · regulatory · fda · via acetaminophen

  2. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA040419)

    fda · regulatory · fda · via acetaminophen

  3. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA087508)

    fda · regulatory · fda · via acetaminophen

  4. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA089805)

    fda · regulatory · fda · via acetaminophen

  5. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA089828)

    fda · regulatory · fda · via acetaminophen

  6. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA089990)

    fda · regulatory · fda · via acetaminophen

  7. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA202800)

    fda · regulatory · fda · via acetaminophen

  8. Supplemental approval2026-06-18

    Supplemental approval: ACETAMINOPHEN AND CODEINE PHOSPHATE (ANDA211610)

    fda · regulatory · fda · via acetaminophen

  9. New publication2023-07-26
    Capsaicin, The Vanilloid Receptor TRPV1 Agonist in Neuroprotection: Mechanisms Involved and Significance.

    Neurochemical research · 2023 · 42 citations · Europe PMC · via Capsaicin

  10. New publication2019-10-25
    Comparison of clinical outcomes of acetaminophen IV vs PO in the peri-operative setting for laparoscopic inguinal hernia repair surgeries: A triple-blinded, randomized controlled trial.

    Journal of clinical anesthesia · 2020 · 13 citations · Europe PMC · via acetaminophen

  11. New publication2011-06-17
    A randomized placebo-controlled trial of acetaminophen for prevention of post-vaccination fever in infants.

    PloS one · 2011 · 16 citations · Europe PMC · via acetaminophen

  12. New publication2010-12-01
    A randomized, double-blind, placebo-controlled, multicenter, repeat-dose study of two intravenous acetaminophen dosing regimens for the treatment of pain after abdominal laparoscopic surgery.

    Clinical therapeutics · 2010 · 93 citations · Europe PMC · via acetaminophen

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.