Target family: Tachykinin receptors (type: gpcr)
Target: NK<sub>3</sub> receptor

Ligand: eledoisin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
Published in: J Biol Chem

Ligand: eledoisin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular characterisation, expression and localisation of human neurokinin-3 receptor.
Published in: FEBS Lett

Ligand: fezolinetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & UK (2023)
Primary target: yes
Median affinity: 7.599999904632568 pKi
Reference (Journal): Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Published in: ACS Med Chem Lett

Ligand: FK 224 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity.
Published in: J Pharmacol Exp Ther

Ligand: GR138676 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): GR138676, a novel peptidic tachykinin antagonist which is potent at NK3 receptors.
Published in: Neuropeptides

Ligand: GSK 172981 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): New quinoline NK3 receptor antagonists with CNS activity.
Published in: Bioorg Med Chem Lett

Ligand: GSK 172981 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.11 pKi
Reference (Journal): In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics.
Published in: Eur J Pharmacol

Ligand: GSK 256471 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.08 pKi
Reference (Journal): In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics.
Published in: Eur J Pharmacol

Ligand: GSK 256471 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): New quinoline NK3 receptor antagonists with CNS activity.
Published in: Bioorg Med Chem Lett

Ligand: hemokinin 1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: hemokinin 1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: kassinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
Published in: J Biol Chem

Ligand: N',2-diphenylquinoline-4-carbohydrazide 8m (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
Published in: Bioorg Med Chem Lett

Ligand: N′,2-diphenylquinoline-4-carbohydrazide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pEC50
Reference (Journal): Molecular characterisation, expression and localisation of human neurokinin-3 receptor.
Published in: FEBS Lett

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: neurokinin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J 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 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): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pEC50
Reference (Journal): Molecular characterisation, expression and localisation of human neurokinin-3 receptor.
Published in: FEBS Lett

Ligand: neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pEC50
Reference (Journal): Antagonists for the neurokinin NK-3 receptor evaluated in selective receptor systems.
Published in: Regul Pept

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Published in: Mol Pharmacol

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Published in: Mol Pharmacol

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
Published in: J Biol Chem

Ligand: osanetant (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: osanetant (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: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.96 pKi
Reference (Journal): SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.
Published in: Life Sci

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Potency and selectivity of the tachykinin NK3 receptor antagonist SR 142801.
Published in: Eur J Pharmacol

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.
Published in: Life Sci

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Osanetant Sanofi-Synthélabo.
Published in: Curr Opin Investig Drugs

Ligand: osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells.
Published in: J Pharmacol Exp Ther

Ligand: pavinetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Webpage): AZD2624.

Ligand: PD 154740 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Published in: Mol Pharmacol

Ligand: PD 154740 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Published in: Mol Pharmacol

Ligand: PD157672 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Published in: Mol Pharmacol

Ligand: PD157672 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
Published in: J Med Chem

Ligand: PD157672 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
Published in: J Biol Chem

Ligand: PD 161182 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.15 pIC50
Reference (Journal): Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
Published in: J Med Chem

Ligand: [Phe(Me)7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: [Phe(Me)7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: [Phe(Me)7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pEC50
Reference (Journal): Antagonists for the neurokinin NK-3 receptor evaluated in selective receptor systems.
Published in: Regul Pept

Ligand: [Phe(Me)7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pEC50
Reference (Journal): Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor.
Published in: Mol Pharmacol

Ligand: [Phe(Me)7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
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: [Pro7]neurokinin B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
Published in: J Biol Chem

Ligand: saredutant (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: saredutant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): The non-peptide tachykinin NK2 receptor antagonist SR 48968 interacts with human, but not rat, cloned tachykinin NK3 receptors.
Published in: Biochem Biophys Res Commun

Ligand: saredutant (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: SB 218795 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.
Published in: J Med Chem

Ligand: SB 222200 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: SB 222200 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: SB 222200 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: SB 235375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.
Published in: J Pharmacol Exp Ther

Ligand: SCH 206272 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 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: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
Published in: J Biol Chem

Ligand: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
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: senktide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.3 pEC50
Reference (Journal): Highly selective agonists for substance P receptor subtypes.
Published in: EMBO J

Ligand: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of a neurokinin B receptor site in rat brain using a highly selective radioligand.
Published in: J Biol Chem

Ligand: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular characterisation, expression and localisation of human neurokinin-3 receptor.
Published in: FEBS Lett

Ligand: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Characterization of a neurokinin B receptor site in rat brain using a highly selective radioligand.
Published in: J Biol Chem

Ligand: senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: SSR 146977 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Biochemical and pharmacological activities of SSR 146977, a new potent nonpeptide tachykinin NK3 receptor antagonist.
Published in: Can J Physiol Pharmacol

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

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][MePhe7]NKB (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]osanetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.899999618530273 pKd

Ligand: [3H]senktide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Pharmacological analysis of [3H]-senktide binding to NK3 tachykinin receptors in guinea-pig ileum longitudinal muscle-myenteric plexus and cerebral cortex membranes.
Published in: Br J Pharmacol

Ligand: talnetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.
Published in: J Med Chem

Ligand: talnetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: talnetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
Published in: Eur J Pharmacol

Ligand: talnetant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological evaluation of novel fluoro and iodo quinoline carboxamides as potential ligands of NK-3 receptors for in vivo imaging studies.
Published in: Bioorg Med Chem

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: [Trp7, β-Ala8] neurokinin A-(4-10) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.46 pA2
Reference (Journal): Antagonists for the neurokinin NK-3 receptor evaluated in selective receptor systems.
Published in: Regul Pept