Target family: Tachykinin receptors (type: gpcr)
Target: NK<sub>2</sub> receptor

Ligand: [βAla8]neurokinin A-(4-10) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKd
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: FK-888 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Effect of YM-44781, YM-44778 and YM-49598, novel tachykinin antagonists, in a drug-induced bladder contraction model.
Published in: Pharmacology

Ligand: GR100679 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Characterisation, CNS distribution and function of NK2 receptors studied using potent NK2 receptor antagonists.
Published in: Regul Pept

Ligand: GR 159897 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: GR 159897 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.
Published in: J Med Chem

Ligand: GR 159897 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors.
Published in: Eur J Pharmacol

Ligand: GR64349 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.
Published in: J Med Chem

Ligand: GR94800 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pKi
Reference (Journal): Synthesis and characterization of selective fluorescent ligands for the neurokinin NK2 receptor.
Published in: J Med Chem

Ligand: hemokinin 1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pKi
Reference (Journal): Pharmacological profile of the novel mammalian tachykinin, hemokinin 1.
Published in: Br J Pharmacol

Ligand: ibodutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): MEN15596, a novel nonpeptide tachykinin NK2 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: [Lys5,Me-Leu9,Nle10]NKA-(4-10) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): An investigation of tachykinin NK2 receptor subtypes in the rat.
Published in: Eur J Pharmacol

Ligand: MEN 10376 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: MEN10627 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists.
Published in: J Med Chem

Ligand: nepadutant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): MEN 11420 (Nepadutant), a novel glycosylated bicyclic peptide tachykinin NK2 receptor antagonist.
Published in: Br J Pharmacol

Ligand: nepadutant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): MEN15596, a novel nonpeptide tachykinin NK2 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of the novel mammalian tachykinin, hemokinin 1.
Published in: Br J Pharmacol

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structure-activity relationships of neurokinin A (4-10) at the human tachykinin NK(2) receptor: the role of natural residues and their chirality.
Published in: Biochem Pharmacol

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.89 pEC50
Reference (Journal): Different receptors are involved in the endothelium-mediated relaxation and the smooth muscle contraction of the rabbit pulmonary artery in response to substance P and related neurokinins.
Published in: Eur J Pharmacol

Ligand: neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: neuropeptide γ (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pEC50
Reference (Journal): Comparison of the effects of neuropeptide K and neuropeptide gamma with neurokinin A at NK2 receptors in the hamster urinary bladder.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: neuropeptide K (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pEC50
Reference (Journal): Comparison of the effects of neuropeptide K and neuropeptide gamma with neurokinin A at NK2 receptors in the hamster urinary bladder.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
Published in: Eur J Pharmacol

Ligand: [Phe(Me)7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: R396 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.25 pIC50
Reference (Journal): Influence of (+/-)-CP-96,345 and SR 48968 on electrical field stimulation of the isolated guinea-pig main bronchus.
Published in: Eur J Pharmacol

Ligand: saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
Published in: Eur J Pharmacol

Ligand: saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor.
Published in: Life Sci

Ligand: saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: SB 414240 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
Published in: J Med Chem

Ligand: SCH 206272 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
Published in: Eur J Pharmacol

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological profile of the novel mammalian tachykinin, hemokinin 1.
Published in: Br J Pharmacol

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of the binding sites of [3H]SR 48968, a potent nonpeptide radioligand antagonist of the neurokinin-2 receptor.
Published in: Biochem Biophys Res Commun

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: [125I]NKA (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Characterization of the [125I]-neurokinin A binding site in the circular muscle of human colon.
Published in: Br J Pharmacol

Ligand: [3H]GR100679 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKd
Reference (Journal): Characterisation, CNS distribution and function of NK2 receptors studied using potent NK2 receptor antagonists.
Published in: Regul Pept

Ligand: [3H]saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Expression of rat NK-2 (neurokinin A) receptor in E. coli.
Published in: Recept Channels

Ligand: talnetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: YM44778 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Effect of YM-44781, YM-44778 and YM-49598, novel tachykinin antagonists, in a drug-induced bladder contraction model.
Published in: Pharmacology

Ligand: YM44781 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.9 pKi
Reference (Journal): Effect of YM-44781, YM-44778 and YM-49598, novel tachykinin antagonists, in a drug-induced bladder contraction model.
Published in: Pharmacology

Ligand: YM49598 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Effect of YM-44781, YM-44778 and YM-49598, novel tachykinin antagonists, in a drug-induced bladder contraction model.
Published in: Pharmacology

Ligand: ZM 253270 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 3.8 pKi
Reference (Journal): Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity.
Published in: J Pharmacol Exp Ther

Ligand: ZM 253270 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.05 pKi
Reference (Journal): Pharmacological characterization of a new class of nonpeptide neurokinin A antagonists that demonstrate species selectivity.
Published in: J Pharmacol Exp Ther

Ligand: ZM-274773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.62 pKi
Reference (Journal): Tachykinin NK2 receptor antagonists. A patent review (2006 - 2010).
Published in: Expert Opin Ther Pat