Target family: Urotensin receptor (type: gpcr)
Target: UT receptor

Ligand: [125I]U-II (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Orphan-receptor ligand human urotensin II: receptor localization in human tissues and comparison of vasoconstrictor responses with endothelin-1.
Published in: Br J Pharmacol

Ligand: tolyacetyl-c[DCys-Apa-DTrp-Orn-Val-Cys]-His-amide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKd
Reference (Journal): Structural requirements at the N-terminus of urotensin II octapeptides.
Published in: Peptides

Ligand: RCI-0879 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Identification of novel Urotensin-II receptor antagonists with potent inhibition of U-II induced pressor response in mice.
Published in: Eur J Pharmacol

Ligand: [Pen5]U-(4-11) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge.
Published in: J Med Chem

Ligand: palosuran (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System.
Published in: J Pharmacol Exp Ther

Ligand: [Orn5]URP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 pKi
Reference (Journal): [Orn5]URP acts as a pure antagonist of urotensinergic receptors in rat cortical astrocytes.
Published in: Peptides

Ligand: JNJ-39319202 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.
Published in: J Med Chem

Ligand: FL104 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Novel and potent small-molecule urotensin II receptor agonists.
Published in: Bioorg Med Chem

Ligand: FL104 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Design, parallel synthesis and SAR of novel urotensin II receptor agonists.
Published in: Eur J Med Chem

Ligand: DS37001789 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pIC50
Reference (Journal): A Novel and Highly Potent Urotensin II Receptor Antagonist Inhibits Urotensin II-Induced Pressure Response in Mice.
Published in: J Cardiovasc Pharmacol

Ligand: compound 1a [PMID: 18573659] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pKi
Reference (Journal): Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
Published in: Bioorg Med Chem Lett

Ligand: [Cha6]U-II-(4-11) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pKi
Reference (Journal): Structure-activity relationships of a novel series of urotensin II analogues: identification of a urotensin II antagonist.
Published in: J Med Chem

Ligand: [Bz-Phe6]U-II (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Photolabelling the rat urotensin II/GPR14 receptor identifies a ligand-binding site in the fourth transmembrane domain.
Published in: Biochem J

Ligand: BIM 23127 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKd
Reference (Journal): The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors.
Published in: Br J Pharmacol

Ligand: AC-7954 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pKi
Reference (Journal): Isochromanone-based urotensin-II receptor agonists.
Published in: Bioorg Med Chem

Ligand: AC-7954 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pKi
Reference (Journal): Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).
Published in: J Med Chem

Ligand: 4-Cl-cinnamoyl-c[DCys-4Pal-DTrp-Orn-Val-Cys]-His-amide (Peptide)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.4 pKd
Reference (Journal): Structural requirements at the N-terminus of urotensin II octapeptides.
Published in: Peptides

Ligand: [3-iodo-Tyr6]U-II-(4-11) (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pEC50
Reference (Journal): Structure-activity relationships of human urotensin II and related analogues on rat aortic ring contraction.
Published in: J Enzyme Inhib Med Chem

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: SB-706375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: SB-706375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: SB-611812 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pKi
Reference (Journal): A role for urotensin II in restenosis following balloon angioplasty: use of a selective UT receptor blocker.
Published in: J Mol Cell Cardiol

Ligand: SB-436811 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKi
Reference (Journal): Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: S6716 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Identification of nonpeptidic urotensin II receptor antagonists by virtual screening based on a pharmacophore model derived from structure-activity relationships and nuclear magnetic resonance studies on urotensin II.
Published in: J Med Chem

Ligand: urotensin II-related peptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): Another ligand fishing for G protein-coupled receptor 14. Discovery of urotensin II-related peptide in the rat brain.
Published in: Peptides

Ligand: urotensin II-related peptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): Characterization of urotensin II, distribution of urotensin II, urotensin II-related peptide and UT receptor mRNAs in mouse: evidence of urotensin II at the neuromuscular junction.
Published in: J Neurochem

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Urotensin II is the endogenous ligand of a G-protein-coupled orphan receptor, SENR (GPR14).
Published in: Biochem Biophys Res Commun

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
Published in: Nature

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Identification of urotensin II as the endogenous ligand for the orphan G-protein-coupled receptor GPR14.
Published in: Biochem Biophys Res Commun

Ligand: urotensin II-related peptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Identification of urotensin II-related peptide as the urotensin II-immunoreactive molecule in the rat brain.
Published in: Biochem Biophys Res Commun

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of genes encoding urotensin-II peptides and their cognate G-protein-coupled receptors from the mouse and monkey.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of genes encoding urotensin-II peptides and their cognate G-protein-coupled receptors from the mouse and monkey.
Published in: Br J Pharmacol

Ligand: U-II-(4-11) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge.
Published in: J Med Chem

Ligand: urantide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): Urantide, an ultrapotent urotensin II antagonist peptide in the rat aorta.
Published in: Br J Pharmacol

Ligand: Urolinin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pEC50
Reference (Journal): Urolinin: The First Linear Peptidic Urotensin-II Receptor Agonist.
Published in: J Med Chem

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Identification of the natural ligand of an orphan G-protein-coupled receptor involved in the regulation of vasoconstriction.
Published in: Nat Cell Biol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Molecular and pharmacological characterization of genes encoding urotensin-II peptides and their cognate G-protein-coupled receptors from the mouse and monkey.
Published in: Br J Pharmacol

Ligand: urotensin-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: SB-706375 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Published in: Br J Pharmacol

Ligand: SR101099 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Potential Therapeutic Value of Urotensin II Receptor Antagonist in Chronic Kidney Disease and Associated Comorbidities.
Published in: J Pharmacol Exp Ther

Ligand: [125I]N-biotin-[Ahx0, Bpa3]U-II (human) (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Biochemical and pharmacological characterization of nuclear urotensin-II binding sites in rat heart.
Published in: Br J Pharmacol

Ligand: [125I]U-II (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
Published in: Nature

Ligand: [125I]U-II (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Molecular and pharmacological characterization of genes encoding urotensin-II peptides and their cognate G-protein-coupled receptors from the mouse and monkey.
Published in: Br J Pharmacol

Ligand: [125I]U-II (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Structure-activity relationships of a novel series of urotensin II analogues: identification of a urotensin II antagonist.
Published in: J Med Chem

Ligand: [125I]U-II (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
Published in: Nature