Target family: Neurotensin receptors (type: gpcr)
Target: NTS<sub>1</sub> receptor

Ligand: Thr10contulakin-G (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Contulakin-G, an O-glycosylated invertebrate neurotensin.
Published in: J Biol Chem

Ligand: Thr10contulakin-G (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): Contulakin-G, an O-glycosylated invertebrate neurotensin.
Published in: J Biol Chem

Ligand: [3H]meclinertant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKd
Reference (Journal): [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor.
Published in: Mol Pharmacol

Ligand: [125I]neurotensin (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus.
Published in: Mol Pharmacol

Ligand: [125I]neurotensin (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor.
Published in: Mol Pharmacol

Ligand: SR48527 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor.
Published in: Mol Pharmacol

Ligand: SR142948A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pIC50
Reference (Journal): Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: neurotensin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A single amino acid of the human and rat neurotensin receptors (subtype 1) determining the pharmacological profile of a species-selective neurotensin agonist.
Published in: Biochem Pharmacol

Ligand: neurotensin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist.
Published in: J Biol Chem

Ligand: neurotensin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A single amino acid of the human and rat neurotensin receptors (subtype 1) determining the pharmacological profile of a species-selective neurotensin agonist.
Published in: Biochem Pharmacol

Ligand: neurotensin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus.
Published in: Mol Pharmacol

Ligand: neurotensin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2.
Published in: Mol Pharmacol

Ligand: neuromedin N (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus.
Published in: Mol Pharmacol

Ligand: meclinertant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist.
Published in: J Biol Chem

Ligand: meclinertant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: meclinertant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor.
Published in: Mol Pharmacol

Ligand: meclinertant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2.
Published in: Mol Pharmacol

Ligand: large neurotensin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Production of recombinant large proneurotensin/neuromedin N-derived peptides and characterization of their binding and biological activity.
Published in: Biochem Biophys Res Commun

Ligand: large neuromedin N (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Production of recombinant large proneurotensin/neuromedin N-derived peptides and characterization of their binding and biological activity.
Published in: Biochem Biophys Res Commun

Ligand: KH28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.92 pIC50
Reference (Journal): Design, synthesis, and evaluation of the antipsychotic potential of orally bioavailable neurotensin (8-13) analogues containing non-natural arginine and lysine residues.
Published in: Neuropharmacology