Target family: Angiotensin receptors (type: gpcr)
Target: AT<sub>1</sub> receptor

Ligand: 5-butyl-methyl immidazole carboxylate 30 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.829999923706055 pA2
Reference (Journal): The discovery of new potent non-peptide Angiotensin II AT1 receptor blockers: a concise synthesis, molecular docking studies and biological evaluation of N-substituted 5-butylimidazole derivatives.
Published in: Eur J Med Chem

Ligand: valsartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2012)
Primary target: yes
Median affinity: 8.609999656677246 pIC50
Reference (Journal): Binding of valsartan to mammalian angiotensin AT1 receptors.
Published in: Regul Pept

Ligand: TRV027 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pKd
Reference (Journal): Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.
Published in: J Pharmacol Exp Ther

Ligand: TRV026 (Peptide)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pKi
Reference (Journal): Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations.
Published in: Cell

Ligand: TRV023 (Peptide)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 5.679999828338623 pEC50
Reference (Patent): β-arrestin effectors and compositions and methods of use thereof

Ligand: TRV023 (Peptide)
Interaction type: Agonist
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 8.640000343322754 pKi
Reference (Journal): Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations.
Published in: Cell

Ligand: telmisartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1998)
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Telmisartan.
Published in: Drugs

Ligand: tasosartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.920000076293945 pIC50
Reference (Journal): Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding.
Published in: J Pharmacol Exp Ther

Ligand: [3H]valsartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Interaction between the partially insurmountable antagonist valsartan and human recombinant angiotensin II type 1 receptors.
Published in: Fundam Clin Pharmacol

Ligand: [3H]losartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.21 pKd
Reference (Journal): Characterization of [3H]losartan receptors in isolated rat glomeruli.
Published in: Eur J Pharmacol

Ligand: [3H]L158809 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.180000305175781 pKd
Reference (Journal): Characterization of the binding of [3H]L-158,809: a new potent and selective nonpeptide angiotensin II receptor (AT1) antagonist radioligand.
Published in: Mol Pharmacol

Ligand: [3H]irbesartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.710000038146973 pKd
Reference (Journal): Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptors.
Published in: J Renin Angiotensin Aldosterone Syst

Ligand: [3H]eprosartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
Reference (Journal): Characterization of [3H]SK&amp;F 108566 as a radioligand for angiotensin type-1 receptor.
Published in: J Recept Res

Ligand: [3H]candesartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.289999961853027 pKd
Reference (Journal): Binding of the antagonist [3H]candesartan to angiotensin II AT1 receptor-transfected [correction of tranfected] Chinese hamster ovary cells.
Published in: Eur J Pharmacol

Ligand: [3H]A81988 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.239999771118164 pKd
Reference (Journal): [3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors.
Published in: Eur J Pharmacol

Ligand: [125I][Sar1,Ile8]Ang-II (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.430000305175781 pKd
Reference (Journal): The docking of Arg2 of angiotensin II with Asp281 of AT1 receptor is essential for full agonism.
Published in: J Biol Chem

Ligand: [125I][Sar1]Ang-II (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.479999542236328 pKd
Reference (Journal): The docking of Arg2 of angiotensin II with Asp281 of AT1 receptor is essential for full agonism.
Published in: J Biol Chem

Ligand: [125I]EXP985 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.829999923706055 pKd
Reference (Journal): [125I]EXP985: a highly potent and specific nonpeptide radioligand antagonist for the AT1 angiotensin receptor.
Published in: Biochem Biophys Res Commun

Ligand: sparsentan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2023)
Primary target: yes
Median affinity: 9.100000381469727 pKi
Reference (Journal): Designed multiple ligands. An emerging drug discovery paradigm.
Published in: J Med Chem

Ligand: [Sar1,Ile8]Ang-II (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.819999694824219 pEC50
Reference (Journal): Interaction of Phe8 of angiotensin II with Lys199 and His256 of AT1 receptor in agonist activation.
Published in: J Biol Chem

Ligand: [Sar1,Ile8]Ang-II (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.430000305175781 pKd
Reference (Journal): Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors.
Published in: Mol Pharmacol

Ligand: [Sar1,Ile4,Ile8]Ang-II (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.510000228881836 pKd
Reference (Journal): Independent beta-arrestin 2 and G protein-mediated pathways for angiotensin II activation of extracellular signal-regulated kinases 1 and 2.
Published in: Proc Natl Acad Sci USA

Ligand: [Sar1,Gly4,Gly8]Ang-II (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.510000228881836 pKd
Reference (Journal): Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors.
Published in: Mol Pharmacol

Ligand: [Sar1,Cha8]Ang-II (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.329999923706055 pKd
Reference (Journal): Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors.
Published in: Mol Pharmacol

Ligand: [Sar1,Cha8]Ang-II (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.329999923706055 pKd
Reference (Journal): Role of aromaticity of agonist switches of angiotensin II in the activation of the AT1 receptor.
Published in: J Biol Chem

Ligand: [Sar1,Cha4]Ang-II (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pKd
Reference (Journal): Role of aromaticity of agonist switches of angiotensin II in the activation of the AT1 receptor.
Published in: J Biol Chem

Ligand: [Sar1,Cha4]Ang-II (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pKd
Reference (Journal): Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors.
Published in: Mol Pharmacol

Ligand: [Sar1,Ala8]Ang-II (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.050000190734863 pKd
Reference (Journal): Side-chain substitutions within angiotensin II reveal different requirements for signaling, internalization, and phosphorylation of type 1A angiotensin receptors.
Published in: Mol Pharmacol

Ligand: saprisartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Pharmacological effects of GR138950, a novel angiotensin AT1 receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: olmesartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2002)
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): In vitro and in vivo pharmacology of olmesartan medoxomil, an angiotensin II type AT1 receptor antagonist.
Published in: J Hypertens Suppl

Ligand: N,N`-bis-alkyl butylimmidazole 12b (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.069999694824219 pIC50
Reference (Journal): Rational design, efficient syntheses and biological evaluation of N,N'-symmetrically bis-substituted butylimidazole analogs as a new class of potent Angiotensin II receptor blockers.
Published in: Eur J Med Chem

Ligand: LY303336 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pIC50
Reference (Journal): Inhibition of angiotensin II-induced inositol phosphate production by triacid nonpeptide antagonists in CHO cells expressing human AT1 receptors.
Published in: Pharm Res

Ligand: LY301875 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.229999542236328 pIC50
Reference (Journal): Inhibition of angiotensin II-induced inositol phosphate production by triacid nonpeptide antagonists in CHO cells expressing human AT1 receptors.
Published in: Pharm Res

Ligand: losartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Angiotensin II receptors and angiotensin II receptor antagonists.
Published in: Pharmacol Rev

Ligand: losartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity:  pIC50
Reference (Book): Heterogeneity of angiotensin receptor subtypes.
Published in: Medicinal Chemistry of the Renin-Angiotensin System.

Ligand: L-163,101 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Structural model of antagonist and agonist binding to the angiotensin II, AT1 subtype, G protein coupled receptor.
Published in: Chem Biol

Ligand: L-162,313 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Non-peptide angiotensin agonist. Functional and molecular interaction with the AT1 receptor.
Published in: J Biol Chem

Ligand: irbesartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (1997)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors.
Published in: Br J Pharmacol

Ligand: forasartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pIC50
Reference (Journal): Pharmacology of SC-52458, an orally active, nonpeptide angiotensin AT1 receptor antagonist.
Published in: J Cardiovasc Pharmacol

Ligand: EXP3174 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Angiotensin II receptors and angiotensin II receptor antagonists.
Published in: Pharmacol Rev

Ligand: EXP3174 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors.
Published in: Br J Pharmacol

Ligand: eprosartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&amp;F 108566.
Published in: J Pharmacol Exp Ther

Ligand: compound 2 [PMID: 28379944] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 pKi
Reference (Journal): Structural basis for selectivity and diversity in angiotensin II receptors.
Published in: Nature

Ligand: compound 1 [PMID: 28379944] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.739999771118164 pKi
Reference (Journal): Structural basis for selectivity and diversity in angiotensin II receptors.
Published in: Nature

Ligand: candesartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors.
Published in: Br J Pharmacol

Ligand: azilsartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Efficacy and safety of 10-mg azilsartan compared with 8-mg candesartan cilexetil in Japanese patients with hypertension: a randomized crossover non-inferiority trial.
Published in: Hypertens Res

Ligand: azilsartan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Evaluation of the efficacy and tolerability of fixed-dose combination therapy of azilsartan and amlodipine besylate in Japanese patients with grade I to II essential hypertension.
Published in: Clin Ther

Ligand: angiotensin IV (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pEC50
Reference (Journal): Angiotensin IV is a potent agonist for constitutive active human AT1 receptors. Distinct roles of the N-and C-terminal residues of angiotensin II during AT1 receptor activation.
Published in: J Biol Chem

Ligand: angiotensin III (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
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:  pIC50
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:  pIC50
Reference (Journal): Distinction between surmountable and insurmountable selective AT1 receptor antagonists by use of CHO-K1 cells expressing human angiotensin II AT1 receptors.
Published in: Br J Pharmacol

Ligand: angiotensin A (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.539999961853027 pIC50
Reference (Journal): Mass-spectrometric identification of a novel angiotensin peptide in human plasma.
Published in: Arterioscler Thromb Vasc Biol

Ligand: angiotensin A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.170000076293945 pEC50
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: Full agonist
Ligand approved: no
Median affinity: 8.800000190734863 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: 5-oxo-1-2-4-oxadiazol biphenyl (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect.
Published in: Bioorg Med Chem

Ligand: 5-oxo-1-2-4-oxadiazol biphenyl (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.989999771118164 pKi
Reference (Journal): Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect.
Published in: Bioorg Med Chem

Ligand: 5-butyl-methyl immidazole carboxylate 30 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): The discovery of new potent non-peptide Angiotensin II AT1 receptor blockers: a concise synthesis, molecular docking studies and biological evaluation of N-substituted 5-butylimidazole derivatives.
Published in: Eur J Med Chem