Target family: Vasopressin and oxytocin receptors (type: gpcr)
Target: V<sub>2</sub> receptor

Ligand: arginine vasotocin (Peptide)
Interaction type: Agonist
Action: Full agonist
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: arginine vasotocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  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): 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: balovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 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: 9.4399995803833 pKi
Reference (Journal): Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.
Published in: Bioorg Med Chem Lett

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: dAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 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:  pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: DAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: DAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: d[Cha4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 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: 6.3 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[D-Ile2,Ile4,Ala-NH2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: d(CH2)5[D-Ile2,Ile4,Ala-NH29]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-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: d(CH2)5[D-Ile2,Ile4]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: d(CH2)5[D-Ile2,Ile4]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[D-Ile2,Ile4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[D-Ile2,Ile4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[D-Ile2,Val4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: d(CH2)5[D-Ile2,Val4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

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:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: d(CH2)5[Tyr(Et)2,Val4,des-Gly9]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): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

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): 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): 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): 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: 5.2 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: 6.7 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,Tyr-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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): 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:  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): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

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: 8.7 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: desmopressin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity:  pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

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: d[Leu4]AVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 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: 6.6 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 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:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: d[Pen1,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[D-Pal2]AVP (Peptide)
Interaction type: Agonist
Action: Agonist
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: Agonist
Action: Agonist
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: Agonist
Action: Agonist
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: 6.6 pKi
Reference (Journal): [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors.
Published in: Endocrinology

Ligand: d[Val4,DArg8]VP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

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: 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: LIT-001 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.78000020980835 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: lixivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: lixivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.
Published in: J Med Chem

Ligand: LVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: LVP (Peptide)
Interaction type: Agonist
Action: Full agonist
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: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
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: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
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: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: mozavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: 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: Inverse agonist
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: nelivaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.9 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: 6.4 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: 4.5 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
Primary target: no
Median affinity: 7 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): 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): 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): 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: oxytocin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1980)
Median affinity:  pKi
Reference (Journal): Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
Published in: EMBO J

Ligand: [Phaa1,D-Tyr(Et)2,Lys6,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

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,Val4,Lys6,Tyr-NH28,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 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: 6.5 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: 6.6 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: 7.1 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): Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: relcovaptan (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: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  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: relcovaptan (Synthetic organic)
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: relcovaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: Ro5028442 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.519999980926514 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: 9 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: 9.3 pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: satavaptan (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: satavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: satavaptan (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: satavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of SR 121463A, a highly potent and selective, orally active vasopressin V2 receptor antagonist.
Published in: J Clin Invest

Ligand: satavaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: SKF-105494 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

Ligand: [125I]d(CH2)5[D-Ile2,Ile4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [125I]d(CH2)5[D-Ile2,Val4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [125I]d(CH2)5[D-Tyr(Et)2,Ile4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [125I]d(CH2)5[D-Tyr(Et)2,Ile4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [125I]d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [125I]d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [3H]AVP (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 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): 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): Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes.
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): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 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): 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): 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: [3H]dDAVP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Properties of [3H]1-desamino-8-D-arginine vasopressin as a radioligand for vasopressin V2-receptors in rat kidney.
Published in: Endocrinology

Ligand: [3H]desGly-NH2[D-Ile2,Ile4]VP (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity: 8.6 pKd

Ligand: [3H]OT (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKd

Ligand: [3H]SR 121463A (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Identification of residues responsible for the selective binding of peptide antagonists and agonists in the V2 vasopressin receptor.
Published in: J Biol Chem

Ligand: [3H]SR 121463A (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of SR 121463A, a highly potent and selective, orally active vasopressin V2 receptor antagonist.
Published in: J Clin Invest

Ligand: [tBaa1,D-Tyr(Et)2,Val4,Lys6,Arg-NH28,des-Gly9]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
Published in: Endocrinology

Ligand: tolvaptan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2009)
Primary target: yes
Median affinity: 9.369999885559082 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: 8.9 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: [Val4]AVP (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: 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): Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.
Published in: Kidney Int

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): 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): 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): 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 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): 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor.
Published in: Biochem 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): 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): 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): 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: VNA932 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
Published in: Bioorg Med Chem Lett

Ligand: YM 218 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 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: 8.9 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