G protein-coupled estrogen receptor 1

BE0003446ProteinHumansGPER1

G protein-coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. It is acted on by 12 drugs in DrugBank.

Gene name
GPER1
UniProtKB entry
Q99527Swiss-Prot
Cellular location
Nucleus
Residues / weight
375 residues · 42,247 Da
Also known as
CEPR · Chemoattractant receptor-like 2 · CMKRL2 · DRY12 · FEG-1

Resolves to

Protein
UniProtQ99527UniProt nameGPER1_HUMAN
Gene
HGNCHGNC:4485NCBI Gene2852GeneCardsGPER1
Pharmacology
IUPHAR/GtoPdb221KEGGhsa:2852
Structure
PDB8XOFPDB8XOGPDB8XOH
Drugs

What you can answer from here — as of June 19, 2026

12DrugsApproved to experimental, with action, bond type and pharmacological action
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61GO termsFunction, process and component, as structured annotations
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1Pfam domainDomain architecture mapped to Pfam families and clans
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49+ReferencesStructured and connected to the statements they support
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Which approved drugs act on G protein-coupled estrogen receptor 1, how selective are they, and which programs against it are still in active trials?

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