Target family: Kisspeptin receptor (type: gpcr)
Target: kisspeptin receptor

Ligand: [125I]Tyr45-kisspeptin-15 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
Published in: Nature

Ligand: [125I]kisspeptin-54 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
Published in: Nature

Ligand: [125I]kisspeptin-14 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Kisspeptins are novel potent vasoconstrictors in humans, with a discrete localization of their receptor, G protein-coupled receptor 54, to atherosclerosis-prone vessels.
Published in: Endocrinology

Ligand: [125I]kisspeptin-13 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Kisspeptins are novel potent vasoconstrictors in humans, with a discrete localization of their receptor, G protein-coupled receptor 54, to atherosclerosis-prone vessels.
Published in: Endocrinology

Ligand: [125I]kisspeptin-10 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKd
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: peptide 234 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation.
Published in: J Neurosci

Ligand: kisspeptin-9 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
Published in: Nature

Ligand: kisspeptin-54 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-54 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
Published in: Nature

Ligand: kisspeptin-54 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pEC50
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-15 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKi
Reference (Journal): Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
Published in: Nature

Ligand: kisspeptin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-10 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: kisspeptin-10 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor.
Published in: Nature

Ligand: kisspeptin-10 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54.
Published in: J Biol Chem

Ligand: [dY]1KP-10 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): A kisspeptin-10 analog with greater in vivo bioactivity than kisspeptin-10.
Published in: Am J Physiol Endocrinol Metab

Ligand: [d-Tyr-14C]TAK-448 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Investigation of disposition for TAK-448, a synthetic peptide of kisspeptin analog, in rats and dogs using the radiolabeled TAK-448 suitable for pharmacokinetic study.
Published in: Xenobiotica

Ligand: 4-fluorobenzoyl-FGLRW-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pEC50
Reference (Journal): Structure-activity relationship study and NMR analysis of fluorobenzoyl pentapeptide GPR54 agonists.
Published in: Biopolymers

Ligand: TAK-448 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pEC50
Reference (Journal): Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH<sub>2</sub> (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility.
Published in: J Med Chem