Target family: Vasopressin and oxytocin receptors (type: gpcr)
Target: V<sub>1A</sub> receptor

Ligand: 3-N3-Phpa-LVA (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.6 pKi
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: arginine vasotocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: arginine vasotocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

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): 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): 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): Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban.
Published in: J Pept Sci

Ligand: balovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.59000015258789 pKd
Reference (Journal): Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder.
Published in: J Med Chem

Ligand: conivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2005)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: conivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2005)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: dAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.
Published in: Endocrinology

Ligand: dAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 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: DAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: d[Cha4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 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: 5.4 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: 5 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[D-Ile2,Ile4,Ala-NH2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: d(CH2)5[D-Ile2,Ile4,Ala-NH2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[D-Ile2,Ile4,Ala-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.
Published in: Eur J Biochem

Ligand: d(CH2)5[Tyr(Et)2,Val4,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: d(CH2)5[Tyr(Me)2,Arg8]VP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.
Published in: Eur J Biochem

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor.
Published in: Biochem Pharmacol

Ligand: d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: d(CH2)5[Tyr(Me)2,Thr4]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 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: 9.3 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: 9 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-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): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes.
Published in: Br J Pharmacol

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity: 5.6 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): 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: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor.
Published in: Biochem Pharmacol

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: d[Leu4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 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: 5.5 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: 5.4 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[Pen1,Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: d[D-Pal2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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[D-Pal2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: d[D-Pal2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A potent new synthetic analog of vasopressin with relative agonist specificity for the pituitary.
Published in: Endocrinology

Ligand: d[D-Phe2]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.
Published in: Endocrinology

Ligand: dVDAVP (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: dVDAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: F180 (Peptide)
Interaction type: Agonist
Action: Full agonist
Primary target: no
Median affinity:  pKd
Reference (Journal): Pharmacological characterization of F-180: a selective human V(1a) vasopressin receptor agonist of high affinity.
Published in: Br J Pharmacol

Ligand: F180 (Peptide)
Interaction type: Agonist
Action: Full agonist
Primary target: no
Median affinity:  pKd
Reference (Journal): Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.
Published in: Eur J Biochem

Ligand: L023103 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
Published in: J Med Chem

Ligand: LIT-001 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 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: 6.7 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: LVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
Published in: J Pharmacol Exp Ther

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
Published in: J Pharmacol Exp Ther

Ligand: nelivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 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: OH-LVA (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: OPC-21268 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: OPC-51803 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes.
Published in: Br J Pharmacol

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
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:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
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)
Median affinity: 6.1 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)
Median affinity:  pKi
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor.
Published in: Biochem Pharmacol

Ligand: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [Phaa1,D-Tyr(Et)2,Lys6,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: [Phaa1,D-Tyr(Et)2,Lys6,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: [Phaa1,D-Tyr(Et)2,Val4,Lys6,Tyr-NH28,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: [Phaa1,D-Tyr(Et)2,Val4,Lys6,Tyr-NH28,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: [Phaa1,D-Tyr(Me)2,Arg6,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: [Phaa1,D-Tyr2,Val4,Arg6,Arg-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: [Phe3]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 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
Primary target: 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
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.
Published in: Eur J Biochem

Ligand: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: Ro5028442 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 9 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: RWJ-351647 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Characterization of RWJ-351647, a novel nonpeptide vasopressin V2 receptor antagonist.
Published in: Clin Exp Pharmacol Physiol

Ligand: satavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Effects of YM471, a nonpeptide AVP V(1A) and V(2) receptor antagonist, on human AVP receptor subtypes expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells.
Published in: Br J Pharmacol

Ligand: satavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: selepressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pEC50
Reference (Journal): Pharmacological characterization of FE 202158, a novel, potent, selective, and short-acting peptidic vasopressin V1a receptor full agonist for the treatment of vasodilatory hypotension.
Published in: J Pharmacol Exp Ther

Ligand: SRX246 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pKi
Reference (Journal): Azetidinones as vasopressin V1a antagonists.
Published in: Bioorg Med Chem

Ligand: SSR126768A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 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: [125I]3-N3-Phpa-LVA (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.9 pKd
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: [125I]OH-LVA (Peptide)
Interaction type: Antagonist
Action: Antagonist
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: [125I]OH-LVA (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.
Published in: Eur J Biochem

Ligand: [3H]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: [3H]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [3H]AVP (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]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: [3H]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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]OT (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pKd
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: [3H]relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKd
Reference (Journal): Binding of [3H] SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes.
Published in: Biochem Biophys Res Commun

Ligand: [tBaa1,D-Tyr(Et)2,Val4,Lys6,Arg-NH28,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: [Thr4,Gly7]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: [Thr4,Gly7]OT (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: tolvaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2009)
Median affinity: 7.9 pKi
Reference (Journal): OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
Published in: J Pharmacol Exp Ther

Ligand: tolvaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2009)
Median affinity: 6.5 pKi
Reference (Journal): OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
Published in: J Pharmacol Exp Ther

Ligand: [Val4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 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: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
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: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes.
Published in: Br J Pharmacol

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding.
Published in: Eur J Biochem

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.
Published in: J Pharmacol Exp Ther

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
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: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor.
Published in: J Biol Chem

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Median affinity: 8.4 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: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
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: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist.
Published in: J Biol Chem

Ligand: vasopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (date of approval not specified)
Primary target: yes
Median affinity:  pKi
Reference (Journal): 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor.
Published in: Biochem Pharmacol

Ligand: YM 218 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors.
Published in: Pharmacol Res

Ligand: YM 471 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Effects of YM471, a nonpeptide AVP V(1A) and V(2) receptor antagonist, on human AVP receptor subtypes expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells.
Published in: Br J Pharmacol