Target family: Gonadotrophin-releasing hormone receptors (type: gpcr)
Target: GnRH<sub>1</sub> receptor

Ligand: WAY-207024 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.15 pIC50
Reference (Journal): Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Published in: J Med Chem

Ligand: WAY-207024 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.92 pIC50
Reference (Journal): Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Published in: J Med Chem

Ligand: [Tyr8]GnRH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Structural determinants for ligand-receptor conformational selection in a peptide G protein-coupled receptor.
Published in: J Biol Chem

Ligand: [Trp8]GnRH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Structural determinants for ligand-receptor conformational selection in a peptide G protein-coupled receptor.
Published in: J Biol Chem

Ligand: triptorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2001)
Median affinity:  pKi
Reference (Journal): Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.
Published in: Biochem Biophys Res Commun

Ligand: triptorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2001)
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.
Published in: Biochem Biophys Res Commun

Ligand: T-98475 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
Published in: J Med Chem

Ligand: [3H]NBI-49202 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism.
Published in: Biochem Pharmacol

Ligand: [125I][Tyr5,DAla6,NMeLeu7,Pro9-NEt]GnRH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pKd
Reference (Journal): Gonadotropin-releasing hormone binding to rat anterior pituitary membrane homogenates. Comparison of antagonists and agonists using radiolabeled antagonist and agonist.
Published in: Mol Pharmacol

Ligand: [125I]triptorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Rat gonadotropin-releasing hormone receptor expressed in insect cells induces activation of adenylyl cyclase.
Published in: Mol Cell Endocrinol

Ligand: [125I]GnRH I (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: [125I][des-Gly10,D-Ala6]GnRH N-ethylamide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats.
Published in: J Pharmacol Exp Ther

Ligand: [125I]cetrorelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKd
Reference (Journal): Residues within transmembrane helices 2 and 5 of the human gonadotropin-releasing hormone receptor contribute to agonist and antagonist binding.
Published in: Mol Endocrinol

Ligand: [125I]buserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKd
Reference (Journal): Stable transfection of GH3 cells with rat gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid results in expression of a receptor coupled to cyclic adenosine 3',5'-monophosphate-dependent prolactin release via a G-protein.
Published in: Endocrinology

Ligand: sufugolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10 pKi
Reference (Journal): Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
Published in: J Med Chem

Ligand: [Ser8]GnRH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): Structural determinants for ligand-receptor conformational selection in a peptide G protein-coupled receptor.
Published in: J Biol Chem

Ligand: relugolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Median affinity: 9.48 pIC50
Reference (Journal): Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Published in: J Med Chem

Ligand: relugolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Median affinity: 9.48 pIC50
Reference (Journal): Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Published in: J Med Chem

Ligand: NBI-42902 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: NBI-42902 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: nafarelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  -

Ligand: merigolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pIC50
Reference (Journal): Effect of SKI2670, a novel, orally active, non-peptide GnRH antagonist, on hypothalamic-pituitary-gonadal axis.
Published in: Life Sci

Ligand: linzagolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2022)
Primary target: no
Median affinity: 7.440000057220459 pIC50
Reference (Journal): Pharmacological characterization of linzagolix, a novel, orally active, non-peptide antagonist of gonadotropin-releasing hormone receptors.
Published in: Clin Exp Pharmacol Physiol

Ligand: linzagolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2022)
Primary target: no
Median affinity: 6.349999904632568 pIC50
Reference (Journal): Pharmacological characterization of linzagolix, a novel, orally active, non-peptide antagonist of gonadotropin-releasing hormone receptors.
Published in: Clin Exp Pharmacol Physiol

Ligand: leuprolide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: leuprolide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1985)
Median affinity: 9.1 pIC50
Reference (Journal): Stable transfection of GH3 cells with rat gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid results in expression of a receptor coupled to cyclic adenosine 3',5'-monophosphate-dependent prolactin release via a G-protein.
Published in: Endocrinology

Ligand: iturelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.46 pKi
Reference (Journal): Gonadotropin releasing hormone antagonists: novel structures incorporating N omega-cyano modified guanidine moieties.
Published in: Biochem Biophys Res Commun

Ligand: iturelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.98 pIC50
Reference (Journal): GnRH and GnRH receptor genes in the human genome.
Published in: Endocrinology

Ligand: IN-3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.77 pIC50
Reference (Journal): Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Published in: Bioorg Med Chem Lett

Ligand: IN-3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.22 pIC50
Reference (Journal): Rescue of hypogonadotropic hypogonadism-causing and manufactured GnRH receptor mutants by a specific protein-folding template: misrouted proteins as a novel disease etiology and therapeutic target.
Published in: J Clin Endocrinol Metab

Ligand: IN-3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.22 pIC50
Reference (Journal): Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Published in: Bioorg Med Chem Lett

Ligand: histrelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: no
Median affinity:  -

Ligand: histerelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: histerelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: [His5,D-Tyr6]GnRH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: goserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  -

Ligand: GnRH III (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKd
Reference (Journal): Structure, enzymatic stability and antitumor activity of sea lamprey GnRH-III and its dimer derivatives.
Published in: Peptides

Ligand: GnRH II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Structural determinants for ligand-receptor conformational selection in a peptide G protein-coupled receptor.
Published in: J Biol Chem

Ligand: GnRH II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification of a novel ligand binding residue Arg38(1.35) in the human gonadotropin-releasing hormone receptor.
Published in: Mol Pharmacol

Ligand: GnRH II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): GnRH-II antagonists induce apoptosis in human endometrial, ovarian, and breast cancer cells via activation of stress-induced MAPKs p38 and JNK and proapoptotic protein Bax.
Published in: Cancer Res

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): Molecular cloning and expression of cDNA encoding the murine gonadotropin-releasing hormone receptor.
Published in: J Biol Chem

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.
Published in: Biochem Biophys Res Commun

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Structure-function studies of linear and cyclized peptide antagonists of the GnRH receptor.
Published in: Biochem Biophys Res Commun

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Stable transfection of GH3 cells with rat gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid results in expression of a receptor coupled to cyclic adenosine 3',5'-monophosphate-dependent prolactin release via a G-protein.
Published in: Endocrinology

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.
Published in: Biosens Bioelectron

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pEC50
Reference (Journal): Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.
Published in: Biosens Bioelectron

Ligand: GnRH I (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Structural determinants for ligand-receptor conformational selection in a peptide G protein-coupled receptor.
Published in: J Biol Chem

Ligand: [Gln8]GnRH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): Structural determinants for ligand-receptor conformational selection in a peptide G protein-coupled receptor.
Published in: J Biol Chem

Ligand: ganirelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: no
Median affinity:  -

Ligand: fertirelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: fertirelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: FD-1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Median affinity: 5.3 pIC50
Reference (Journal): Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.
Published in: Mol Pharmacol

Ligand: FD-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Median affinity: 8.3 pKi
Reference (Journal): Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.
Published in: Mol Pharmacol

Ligand: elagolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018)
Primary target: yes
Median affinity: 9.050000190734863 pKi
Reference (Journal): Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
Published in: J Med Chem

Ligand: elagolix (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018)
Primary target: yes
Median affinity: 9.050000190734863 pKi
Reference (Journal): Elagolix: First Global Approval.
Published in: Drugs

Ligand: [D-Lys6]GnRH-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.59 pIC50
Reference (Journal): GnRH-II antagonists induce apoptosis in human endometrial, ovarian, and breast cancer cells via activation of stress-induced MAPKs p38 and JNK and proapoptotic protein Bax.
Published in: Cancer Res

Ligand: deslorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: deslorelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: [des-Gly10,D-Ala6]GnRH N-ethylamide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.9 pIC50
Reference (Journal): Molecular cloning and expression of cDNA encoding the murine gonadotropin-releasing hormone receptor.
Published in: J Biol Chem

Ligand: degarelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2009)
Primary target: yes
Median affinity: 8.770000457763672 pKi
Reference (Journal): Evaluation of degarelix in the management of prostate cancer.
Published in: Cancer Manag Res

Ligand: D-24710 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay.
Published in: Anal Biochem

Ligand: D-23487 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10 pKi
Reference (Journal): Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay.
Published in: Anal Biochem

Ligand: cyclorelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay.
Published in: Anal Biochem

Ligand: compound 4 [PMID: 32677155] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.260000228881836 pKi
Reference (Journal): Discovery of a Lead Brain-Penetrating Gonadotropin-Releasing Hormone Receptor Antagonist with Saturable Binding in Brain.
Published in: ChemMedChem

Ligand: CMPD-1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Allosteric and orthosteric binding modes of two nonpeptide human gonadotropin-releasing hormone receptor antagonists.
Published in: Biochemistry

Ligand: CMPD-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats.
Published in: J Pharmacol Exp Ther

Ligand: cetrorelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (1999), FDA (2000)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Selection and characterization of mammalian cell lines with stable over-expression of human pituitary receptors for gonadoliberin.
Published in: Eur J Biochem

Ligand: cetrorelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (1999), FDA (2000)
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): GnRH and GnRH receptor genes in the human genome.
Published in: Endocrinology

Ligand: cetrorelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (1999), FDA (2000)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay.
Published in: Anal Biochem

Ligand: cetrorelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (1999), FDA (2000)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: buserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pEC50
Reference (Journal): Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.
Published in: Biosens Bioelectron

Ligand: buserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: buserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: buserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity: 10.520000457763672 pEC50
Reference (Journal): Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.
Published in: Biosens Bioelectron

Ligand: buserelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKd
Reference (Journal): Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.
Published in: Biosens Bioelectron

Ligand: BAY1214784 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pIC50
Reference (Journal): Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Published in: J Med Chem

Ligand: antarelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.6 pKi
Reference (Journal): Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay.
Published in: Anal Biochem

Ligand: alarelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: alarelin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in: Br J Pharmacol

Ligand: abarelix (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Published in: Endocrinology

Ligand: 5-(N,N-hexamethylene)-amiloride (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 4.3 pIC50
Reference (Journal): Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.
Published in: Mol Pharmacol