Target family: Endothelin receptors (type: gpcr)
Target: ET<sub>B</sub> receptor

Ligand: [125I]ET-1 (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization and ontogeny of endothelin receptors in human placenta.
Published in: Am J Physiol

Ligand: TAK 044 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pA2
Reference (Journal): Pharmacology of a non-selective ETA and ETB receptor antagonist, TAK-044 and the inhibition of myocardial infarct size in rats.
Published in: Br J Pharmacol

Ligand: [125I]IRL1620 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Species differences in the binding characteristics of [125I]IRL-1620, a potent agonist specific for endothelin-B receptors.
Published in: J Pharmacol Exp Ther

Ligand: [125I]IRL1620 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Species differences in the binding characteristics of [125I]IRL-1620, a potent agonist specific for endothelin-B receptors.
Published in: J Pharmacol Exp Ther

Ligand: [125I]ET-1 (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Novel ligands BQ123 and BQ3020 characterize endothelin receptor subtypes ETA and ETB in human kidney.
Published in: Kidney Int

Ligand: [125I]ET-1 (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Endothelin receptor density in human hypertrophic and non-hypertrophic prostate tissue.
Published in: Tohoku J Exp Med

Ligand: [125I]ET-1 (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Book): Distribution of endothelin receptors.
Published in: Endothelins in Biology and Medicine

Ligand: [125I]ET-1 (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Endothelin ETA and ETB mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ETA sub-type.
Published in: Br J Pharmacol

Ligand: [125I]ET-1 (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Increased capillary permeability to albumin in diabetic rat myocardium.
Published in: Circ Res

Ligand: [125I]BQ3020 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Selectivity of [125I]-PD151242 for human, rat and porcine endothelin ETA receptors in the heart.
Published in: Br J Pharmacol

Ligand: [125I]BQ3020 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of endothelin receptors in human brain cortex, gliomas, and meningiomas.
Published in: J Cardiovasc Pharmacol

Ligand: [125I]BQ3020 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of two new ETB selective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart.
Published in: Br J Pharmacol

Ligand: [125I][Ala1,3,11,15]ET-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Characterization of two new ETB selective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart.
Published in: Br J Pharmacol

Ligand: sovateltide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: India CDSCO (2023)
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): A reversible radioligand specific for the ETB receptor: [125I]Tyr13-Suc-[Glu9,Ala11,15]-endothelin-1(8- 21), [125I]IRL 1620.
Published in: Biochem Biophys Res Commun

Ligand: sovateltide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: India CDSCO (2023)
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Sovateltide Mediated Endothelin B Receptors Agonism and Curbing Neurological Disorders.
Published in: Int J Mol Sci

Ligand: SB209670 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKB
Reference (Journal): 1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.
Published in: J Med Chem

Ligand: sarafotoxin S6c (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: sarafotoxin S6c (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of peptide and nonpeptide antagonists in human kidney.
Published in: J Cardiovasc Pharmacol

Ligand: sarafotoxin S6c (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: sarafotoxin S6c (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: Ro 46-8443 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor.
Published in: FEBS Lett

Ligand: RES7011 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin.
Published in: Mol Pharmacol

Ligand: macitentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2013)
Primary target: no
Median affinity: 6.409999847412109 pIC50
Reference (Journal): The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.
Published in: J Med Chem

Ligand: K-8794 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 pIC50
Reference (Journal): X-ray structures of endothelin ET<sub>B</sub> receptor bound to clinical antagonist bosentan and its analog.
Published in: Nat Struct Mol Biol

Ligand: IRL 2500 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: endothelin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization and ontogeny of endothelin receptors in human placenta.
Published in: Am J Physiol

Ligand: endothelin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Book): Distribution of endothelin receptors.
Published in: Endothelins in Biology and Medicine

Ligand: endothelin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: endothelin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Endothelin receptor density in human hypertrophic and non-hypertrophic prostate tissue.
Published in: Tohoku J Exp Med

Ligand: endothelin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: endothelin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: clazosentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2022)
Primary target: no
Median affinity: 6.760000228881836 pKi
Reference (Journal): Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).
Published in: J Med Chem

Ligand: BQ788 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: BQ788 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKd
Reference (Journal): Characterization of the binding of endothelin ETB selective ligands in human and rat heart.
Published in: Br J Pharmacol

Ligand: BQ 3020 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): Pharmacological differences between rat and human endothelin B receptors.
Published in: Biochem Biophys Res Commun

Ligand: bosentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2001), EMA (2002)
Primary target: yes
Median affinity: 7.099999904632568 pKi
Reference (Journal): Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: bosentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2001), EMA (2002)
Median affinity: 6 pA2
Reference (Journal): Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: BMS-193884 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.730000019073486 pKi
Reference (Journal): Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.
Published in: J Med Chem

Ligand: atrasentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.860000133514404 pKi
Reference (Journal): 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Published in: J Med Chem

Ligand: aprocitentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 6.010000228881836 pIC50
Reference (Journal): Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: aprocitentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 5.5 pA2
Reference (Journal): Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: ambrisentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2007), EMA (2008)
Primary target: no
Median affinity: 5.920000076293945 pIC50
Reference (Journal): Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Published in: J Med Chem

Ligand: [Ala1,3,11,15]ET-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of two new ETB selective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart.
Published in: Br J Pharmacol

Ligand: A192621 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pKd
Reference (Journal): Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.
Published in: J Med Chem