Target family: Angiotensin receptors (type: gpcr)
Target: AT<sub>2</sub> receptor

Ligand: [125I][Sar1,Ile8]Ang-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Intracellular sodium modulates the expression of angiotensin II subtype 2 receptor in PC12W cells.
Published in: Hypertension

Ligand: [125I]CGP42112 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.6 pKd
Reference (Journal): Preliminary biochemical characterization of two angiotensin II receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: [125I]CGP42112 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.6 pKd
Reference (Book): Heterogeneity of angiotensin receptor subtypes.
Published in: Medicinal Chemistry of the Renin-Angiotensin System.

Ligand: [125I]CGP42112 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.6 pKd
Reference (Journal): Radioiodinated CGP 42112A: a novel high affinity and highly selective ligand for the characterization of angiotensin AT2 receptors.
Published in: Biochem Biophys Res Commun

Ligand: saralasin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Identification of angiotensin II receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: PD123319 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Subclasses of angiotensin II binding sites and their functional significance.
Published in: Mol Pharmacol

Ligand: PD123319 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Book): Heterogeneity of angiotensin receptor subtypes.
Published in: Medicinal Chemistry of the Renin-Angiotensin System.

Ligand: PD123319 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of distinct angiotensin II binding sites in rat adrenal gland and bovine cerebellum using selective nonpeptide antagonists.
Published in: J Cardiovasc Pharmacol

Ligand: PD123177 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification of angiotensin II receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: PD123177 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Two distinct angiotensin II receptor binding sites in rat adrenal revealed by new selective nonpeptide ligands.
Published in: Mol Pharmacol

Ligand: PD123177 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Regulated expression of angiotensin II (AT2) binding sites in R3T3 cells.
Published in: Regul Pept

Ligand: [p-aminoPhe6]ang II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Book): Heterogeneity of angiotensin receptor subtypes.
Published in: Medicinal Chemistry of the Renin-Angiotensin System.

Ligand: [p-aminoPhe6]ang II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Discrimination of two angiotensin II receptor subtypes with a selective agonist analogue of angiotensin II, p-aminophenylalanine6 angiotensin II.
Published in: Biochem Biophys Res Commun

Ligand: olodanrigan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.
Published in: Lancet

Ligand: olodanrigan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Small molecule angiotensin II type 2 receptor (AT₂R) antagonists as novel analgesics for neuropathic pain: comparative pharmacokinetics, radioligand binding, and efficacy in rats.
Published in: Pain Med

Ligand: olodanrigan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Angiotensin II: from blood pressure to pain control.
Published in: Lancet

Ligand: olodanrigan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.53000020980835 pIC50
Reference (Journal): Small molecule angiotensin II type 2 receptor (AT₂R) antagonists as novel analgesics for neuropathic pain: comparative pharmacokinetics, radioligand binding, and efficacy in rats.
Published in: Pain Med

Ligand: novokinin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.130000114440918 pKi
Reference (Journal): Hypotensive activity of novokinin, a potent analogue of ovokinin(2-7), is mediated by angiotensin AT(2) receptor and prostaglandin IP receptor.
Published in: Peptides

Ligand: compound 2 [PMID: 28379944] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.460000038146973 pKi
Reference (Journal): Structural basis for selectivity and diversity in angiotensin II receptors.
Published in: Nature

Ligand: compound 21 [PMID: 22802221] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.
Published in: J Med Chem

Ligand: compound 21 [PMID: 22802221] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pEC50
Reference (Journal): Compound 21 induces vasorelaxation via an endothelium- and angiotensin II type 2 receptor-independent mechanism.
Published in: Hypertension

Ligand: compound 21 [PMID: 22802221] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Compound 21 induces vasorelaxation via an endothelium- and angiotensin II type 2 receptor-independent mechanism.
Published in: Hypertension

Ligand: compound 1 [PMID: 28379944] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.470000267028809 pKi
Reference (Journal): Structural basis for selectivity and diversity in angiotensin II receptors.
Published in: Nature

Ligand: CGP42112 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.630000114440918 pIC50
Reference (Journal): Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors.
Published in: Clin Sci

Ligand: angiotensin III (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.399999618530273 pKd
Reference (Journal): Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype.
Published in: Br J Pharmacol

Ligand: angiotensin III (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.399999618530273 pKd
Reference (Journal): Preliminary biochemical characterization of two angiotensin II receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: angiotensin III (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.399999618530273 pKd
Reference (Book): Heterogeneity of angiotensin receptor subtypes.
Published in: Medicinal Chemistry of the Renin-Angiotensin System.

Ligand: angiotensin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2017)
Primary target: no
Median affinity: 10.199999809265137 pKd
Reference (Journal): Human angiotensin receptor subtypes.
Published in: Curr Opin Nephrol Hypertens

Ligand: angiotensin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2017)
Primary target: no
Median affinity: 10.199999809265137 pKd
Reference (Book): Heterogeneity of angiotensin receptor subtypes.
Published in: Medicinal Chemistry of the Renin-Angiotensin System.

Ligand: angiotensin II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2017)
Primary target: no
Median affinity: 10.199999809265137 pKd
Reference (Journal): Preliminary biochemical characterization of two angiotensin II receptor subtypes.
Published in: Biochem Biophys Res Commun

Ligand: angiotensin A (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.640000343322754 pKi
Reference (Journal): Pressor and renal hemodynamic effects of the novel angiotensin A peptide are angiotensin II type 1A receptor dependent.
Published in: Hypertension

Ligand: angiotensin A (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.920000076293945 pIC50
Reference (Journal): Mass-spectrometric identification of a novel angiotensin peptide in human plasma.
Published in: Arterioscler Thromb Vasc Biol

Ligand: angiotensin-(1-7) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.610000133514404 pIC50
Reference (Journal): Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors.
Published in: Clin Sci