Target family: Neuropeptide S receptor (type: gpcr)
Target: NPS receptor

Ligand: [Cy5-Lys19]NPS (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pEC50
Reference (Journal): Human Neuropeptide S Receptor Is Activated via a Gαq Protein-biased Signaling Cascade by a Human Neuropeptide S Analog Lacking the C-terminal 10 Residues.
Published in: J Biol Chem

Ligand: SHA 68 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pA2
Reference (Journal): [tBu-D-Gly5]NPS, a pure and potent antagonist of the neuropeptide S receptor: in vitro and in vivo studies.
Published in: Peptides

Ligand: RTI-118 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identifying structural features on 1,1-diphenyl-hexahydro-oxazolo[3,4-a]pyrazin-3-ones critical for Neuropeptide S antagonist activity.
Published in: Bioorg Med Chem Lett

Ligand: QA1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: PWT1-NPS (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.989999771118164 pEC50
Reference (Journal): In vitro and in vivo pharmacological characterization of a neuropeptide S tetrabranched derivative.
Published in: Pharmacol Res Perspect

Ligand: PI1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Published in: Bioorg Med Chem Lett

Ligand: NPS(1-4)NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation.
Published in: Neuropharmacology

Ligand: NPS(1-4)NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation.
Published in: Neuropharmacology

Ligand: neuropeptide S (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pEC50
Reference (Journal): Neuropeptide S: a neuropeptide promoting arousal and anxiolytic-like effects.
Published in: Neuron

Ligand: neuropeptide S (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.340000152587891 pEC50
Reference (Journal): Neuropeptide S receptor 1 is a nonhormonal treatment target in endometriosis.
Published in: Sci Transl Med

Ligand: neuropeptide S (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pEC50
Reference (Journal): Neuropeptide S: a neuropeptide promoting arousal and anxiolytic-like effects.
Published in: Neuron

Ligand: neuropeptide S (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pEC50
Reference (Journal): Neuropeptide S: a neuropeptide promoting arousal and anxiolytic-like effects.
Published in: Neuron

Ligand: NCGC 84 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.979999542236328 pA2
Reference (Journal): A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats.
Published in: J Neurosci

Ligand: [tBu-D-Gly5]NPS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pA2
Reference (Journal): Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
Published in: J Med Chem

Ligand: [tBu-D-Gly5]NPS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pA2
Reference (Journal): [tBu-D-Gly5]NPS, a pure and potent antagonist of the neuropeptide S receptor: in vitro and in vivo studies.
Published in: Peptides

Ligand: [D-Val5]NPS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKB
Reference (Journal): Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
Published in: J Med Chem

Ligand: [D-Cys(tBu)5]NPS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pA2
Reference (Journal): [tBu-D-Gly5]NPS, a pure and potent antagonist of the neuropeptide S receptor: in vitro and in vivo studies.
Published in: Peptides

Ligand: [D-Cys(tBu)5]NPS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pA2

Ligand: [125I]Tyr10NPS (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Neuropeptide S: a neuropeptide promoting arousal and anxiolytic-like effects.
Published in: Neuron

Ligand: SHA 68R (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.059999942779541 pIC50
Reference (Journal): Neuropeptide S receptor 1 is a nonhormonal treatment target in endometriosis.
Published in: Sci Transl Med

Ligand: SHA 68 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pA2
Reference (Journal): Further studies on the pharmacological profile of the neuropeptide S receptor antagonist SHA 68.
Published in: Peptides