Target family: G protein-coupled estrogen receptor (type: gpcr)
Target: GPER

Ligand: G15 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): In vivo effects of a GPR30 antagonist.
Published in: Nat Chem Biol

Ligand: 2-Methoxyestradiol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKd
Reference (Journal): 2-methoxyestradiol binding of GPR30 down-regulates angiotensin AT(1) receptor.
Published in: Eur J Pharmacol

Ligand: G-1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Virtual and biomolecular screening converge on a selective agonist for GPR30.
Published in: Nat Chem Biol

Ligand: fulvestrant (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
Published in: Endocrinology

Ligand: tamoxifen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 6 pKi
Reference (Journal): Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
Published in: Endocrinology

Ligand: [3H]17β-estradiol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
Published in: Endocrinology

Ligand: raloxifene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997), EMA (1998)
Primary target: no
Median affinity: 7 pKi
Reference (Journal): G protein-coupled estrogen receptor-selective ligands modulate endometrial tumor growth.
Published in: Obstet Gynecol Int

Ligand: 4-hydroxytamoxifen (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A transmembrane intracellular estrogen receptor mediates rapid cell signaling.
Published in: Science

Ligand: G36 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity.
Published in: J Steroid Biochem Mol Biol

Ligand: 17β-estradiol (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1954, prior history unavailable)
Primary target: no
Median affinity:  pKi
Reference (Journal): Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
Published in: Endocrinology

Ligand: 17β-estradiol (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1954, prior history unavailable)
Primary target: no
Median affinity:  pKi
Reference (Journal): A transmembrane intracellular estrogen receptor mediates rapid cell signaling.
Published in: Science