Target family: Vasopressin and oxytocin receptors (type: gpcr)
Target: OT receptor

Ligand: arginine vasotocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: arginine vasotocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.
Published in: FEBS Lett

Ligand: atosiban (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2000)
Median affinity:  pKi
Reference (Journal): Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.
Published in: Br J Obstet Gynaecol

Ligand: atosiban (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2000)
Median affinity:  pKi
Reference (Journal): Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban.
Published in: J Pept Sci

Ligand: atosiban (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2000)
Median affinity:  pKi
Reference (Journal): SSR126768A (4-Chloro-3-[(3R)-(+)-5-chloro-1-(2,4-dimethoxybenzyl)-3-methyl-2oxo-2,3-dihydro-1H-indol-3-yl]-N-ethyl-N-(3-pyridylmethyl)-benzamidine, hydrochloride): a new selective and orally active oxytocin receptor antagonist for the prevention of preterm labor.
Published in: J Pharmacol Exp Therap

Ligand: atosiban (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2000)
Median affinity:  pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: atosiban (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2000)
Median affinity: 7.1 pKi
Reference (Journal): Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Published in: J Pharmacol Exp Ther

Ligand: atosiban (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2000)
Median affinity:  pKi
Reference (Journal): Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Published in: J Pharmacol Exp Ther

Ligand: balovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.150000095367432 pKi
Reference (Journal): Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder.
Published in: J Med Chem

Ligand: carbetocin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: UK (2007)
Primary target: no
Median affinity: 8 pEC50
Reference (Journal): LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Published in: J Med Chem

Ligand: carbetocin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: UK (2007)
Primary target: no
Median affinity: 7.210000038146973 pEC50
Reference (Journal): LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Published in: J Med Chem

Ligand: compound 37 [PMID: 16250654] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): 2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.
Published in: J Med Chem

Ligand: dAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
Published in: J Med Chem

Ligand: d[Cha4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol

Ligand: d[Cha4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.
Published in: Endocrinology

Ligand: d[Cha4,Dab8]VP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Published in: J Med Chem

Ligand: d[Cha4]LVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Published in: J Med Chem

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Phe(3125I,4N3)-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.6 pKd
Reference (Journal): Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Tyr(3125I)-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Tyr(3125I)-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Tyr(3125I)-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.
Published in: FEBS Lett

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban.
Published in: J Pept Sci

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol

Ligand: desGlyNH2-d(CH2)5[Tyr(Me)2,Thr4,Orn8]OT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: d[Leu4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
Published in: J Med Chem

Ligand: d[Leu4,Dap8]VP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Published in: J Med Chem

Ligand: d[Leu4]LVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Published in: J Med Chem

Ligand: L023103 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
Published in: J Med Chem

Ligand: L023103 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
Published in: J Med Chem

Ligand: L-365,209 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-366,509 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-366,682 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-366,875 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-366,948 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-367,773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-367,938 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-368,228 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-368,899 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-368,930 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-369,020 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: L-371,257 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol

Ligand: L-372662 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.
Published in: J Med Chem

Ligand: LIT-001 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.650000095367432 pKi
Reference (Journal): LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Published in: J Med Chem

Ligand: LS-192629 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Published in: J Pharmacol Exp Ther

Ligand: LS-192629 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Published in: J Pharmacol Exp Ther

Ligand: [Mpa1,D-Tyr(Et)2,D-Tic7,Aib9]OT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.
Published in: Eur J Med Chem

Ligand: [Mpa1,D-Tyr(Et)2,D-Tic7]OT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.
Published in: Eur J Med Chem

Ligand: [Mpa1,D-Tyr(Et)2,D-Tic7,D-Tic9]OT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.
Published in: Eur J Med Chem

Ligand: nelivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: nelivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol

Ligand: OPC-21268 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Published in: J Pharmacol Exp Ther

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity: 8.7 pKi
Reference (Journal): Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Published in: J Pharmacol Exp Ther

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.
Published in: Br J Obstet Gynaecol

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.
Published in: FEBS Lett

Ligand: [Phe3]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.
Published in: FEBS Lett

Ligand: [Phe3]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.
Published in: Br J Obstet Gynaecol

Ligand: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol

Ligand: retosiban (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Use of a novel and highly selective oxytocin receptor antagonist to characterize uterine contractions in the rat.
Published in: Am J Physiol Regul Integr Comp Physiol

Ligand: retosiban (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): The discovery of GSK221149A: a potent and selective oxytocin antagonist.
Published in: Bioorg Med Chem Lett

Ligand: Ro5028442 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.
Published in: J Med Chem

Ligand: SSR126768A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): SSR126768A (4-Chloro-3-[(3R)-(+)-5-chloro-1-(2,4-dimethoxybenzyl)-3-methyl-2oxo-2,3-dihydro-1H-indol-3-yl]-N-ethyl-N-(3-pyridylmethyl)-benzamidine, hydrochloride): a new selective and orally active oxytocin receptor antagonist for the prevention of preterm labor.
Published in: J Pharmacol Exp Therap

Ligand: [111In]DOTA-dLVT (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity: 8.3 pKd
Reference (Journal): Improved radiotracing of oxytocin receptor-expressing tumours using the new [111In]-DOTA-Lys8-deamino-vasotocin analogue.
Published in: Br J Cancer

Ligand: [125I]d(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10 pKd

Ligand: [35S]non-peptide OT antagonist (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.380000114440918 pKd
Reference (Journal): A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors.
Published in: Eur J Pharmacol

Ligand: [3H]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: [3H]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: [3H]OT (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: [3H]OT (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Molecular characterization of a cloned human oxytocin receptor.
Published in: Eur J Endocrinol

Ligand: [3H]OT (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: [3H]OT (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Oxytocin receptors and human parturition: a dual role for oxytocin in the initiation of labor.
Published in: Science

Ligand: [Thr4,Gly7]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [3H]-[Thr4,Gly7]OT: a highly selective ligand for central and peripheral OT receptors.
Published in: Am J Physiol

Ligand: [Thr4,Gly7]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.
Published in: FEBS Lett

Ligand: [Thr4,Gly7]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: [Thr4,Gly7]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Selective and potent agonists and antagonists for investigating the role of mouse oxytocin receptors.
Published in: J Pharmacol Exp Ther

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.
Published in: Br J Obstet Gynaecol

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.
Published in: Endocrinology

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
Published in: Life Sci

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin.
Published in: FEBS Lett

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
Published in: J Med Chem

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity:  pKi
Reference (Journal): Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
Published in: Br J Pharmacol