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Protein / target

Gonadotropin-releasing hormone receptor

Encoded byGNRHRP30968Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
22
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Gonadotropin-releasing hormone receptor

Strongest disease association

Hypogonadism

Via encoding gene GNRHR · Genetic evidence · score 0.93

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

Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

View complete UniProt function annotation

Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling

Subcellular location

Cell membrane
Domains and Gene Ontology detail (6)

Gene Ontology

  • Cmembrane
  • Cplasma membrane
  • Fgonadotropin-releasing hormone receptor activity
  • Pcellular response to hormone stimulus
  • PG protein-coupled receptor signaling pathway
  • Pgonadotropin secretion

328 aa · 38 kDa · 2 isoforms

Approved medicines with mapped indications

2 medicines · 2 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.

Infertility, Female1 medicine
Neoplasms1 medicine

22 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.

ganirelix
Narrow target profileApprovedAntagonist

Gonadotropin-releasing hormone receptor antagonist

Indicated for Infertility, Female

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

buserelin
Narrow target profileApprovedAgonist

Gonadotropin-releasing hormone receptor agonist

Indicated for Neoplasms

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

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 GNRHR

Gene-level evidence surfaced through the gene GNRHRthat 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.

Hypogonadism
0.96Well supported

Genetic evidence dominant · Open Targets 0.83

Prostatic Neoplasms
0.75Well supported

Clinical evidence dominant · Open Targets 0.61

Endometriosis
0.73Moderately supported

Clinical evidence dominant · Open Targets 0.59

Prostate carcinoma
0.73Moderately supported

Clinical evidence dominant · Open Targets 0.59

Breast Neoplasms
0.72Moderately supported

Clinical evidence dominant · Open Targets 0.58

View evidence synthesis (5)
HypogonadismWell supported
0.96
agreement 0.861.00
Genetic68%Animal model19%Clinical10%Literature3%Genetic literaturedup

Open Targets aggregate 0.83 · 4 independent evidence families · 1 not counted as duplicate

Prostatic NeoplasmsWell supported
0.75
agreement 0.600.91
Clinical95%Literature5%

Open Targets aggregate 0.61 · 2 independent evidence families

EndometriosisModerately supported
0.73
agreement 0.570.88
Clinical96%Literature4%

Open Targets aggregate 0.59 · 2 independent evidence families

Prostate carcinomaModerately supported
0.73
agreement 0.570.88
Clinical93%Literature7%

Open Targets aggregate 0.59 · 2 independent evidence families

Breast NeoplasmsModerately supported
0.72
agreement 0.570.88
Clinical94%Literature7%

Open Targets aggregate 0.58 · 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
Hypogonadism0.83
Prostatic Neoplasms0.61
Endometriosis0.59
Prostate carcinoma0.59
Breast Neoplasms0.58
Neoplasms0.58
Puberty, Precocious0.56

Drug development

32 compounds recorded · 22 approved · 10 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)
LINZAGOLIX CHOLINEApproval
GONADORELINApproval
RELUGOLIXApproval
HISTRELINApproval
ACYLINEPhase 2
TRIPTORELIN PAMOATEApproval
LINZAGOLIXPhase 3
BUSERELINApproval
DEGARELIXApproval
GOSERELINApproval

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 (go cc high conf and uniprot loc med 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

Approved Drug support this modality.

View underlying tractability evidence (9)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

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)

ACTIVE_NOT_RECRUITING · via ganirelix · NCT04037605

ACTIVE_NOT_RECRUITING · via ganirelix · NCT03142893

ClinicalTrials.gov via the drug-target graph.

What's happening now

1

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.

  1. Regulatory approval2000-05-16

    Approval: Orgalutran (EMA)

    ema · regulatory · ema · via ganirelix

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.