Target family: Leukotriene receptors (type: gpcr)
Target: CysLT<sub>2</sub> receptor

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 5.150000095367432 pIC50
Reference (Journal): Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Published in: Br J Pharmacol

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 5.130000114440918 pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 6.900000095367432 pA2
Reference (Journal): Autocrine activity of cysteinyl leukotrienes in human vascular endothelial cells: Signaling through the CysLT₂ receptor.
Published in: Prostaglandins Other Lipid Mediat

Ligand: [3H]LTD4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: [3H]LTC4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.52 pKd
Reference (Journal): The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor.
Published in: Biochem Biophys Res Commun

Ligand: [3H]LTC4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.54 pKd
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J

Ligand: [3H]LTC4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Identification and characterization of two cysteinyl-leukotriene high affinity binding sites with receptor characteristics in human lung parenchyma.
Published in: Mol Pharmacol

Ligand: [3H]ICI-198615 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 pKd
Reference (Journal): Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.
Published in: Biochem Pharmacol

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 7.099999904632568 pA2
Reference (Journal): Autocrine activity of cysteinyl leukotrienes in human vascular endothelial cells: Signaling through the CysLT₂ receptor.
Published in: Prostaglandins Other Lipid Mediat

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 5.440000057220459 pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: pobilukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pA2
Reference (Journal): Autocrine activity of cysteinyl leukotrienes in human vascular endothelial cells: Signaling through the CysLT₂ receptor.
Published in: Prostaglandins Other Lipid Mediat

Ligand: ONO-2570366 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.
Published in: Nat Commun

Ligand: N-methyl LTC4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.06 pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: N-methyl LTC4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.91 pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor.
Published in: Biochem Biophys Res Commun

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.72 pIC50
Reference (Journal): The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor.
Published in: Biochem Biophys Res Commun

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Identification and characterization of two cysteinyl-leukotriene high affinity binding sites with receptor characteristics in human lung parenchyma.
Published in: Mol Pharmacol

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.46 pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification and characterization of two cysteinyl-leukotriene high affinity binding sites with receptor characteristics in human lung parenchyma.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.15 pIC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.44 pEC50
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.23 pIC50
Reference (Journal): The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor.
Published in: Biochem Biophys Res Commun

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor.
Published in: Biochem Biophys Res Commun

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.24 pEC50
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor.
Published in: Biochem Biophys Res Commun

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.27 pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT₂) agonist, N-methyl-leukotriene C₄, in calcium reporter and β arrestin assays.
Published in: Mol Pharmacol

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: iralukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pA2
Reference (Journal): Autocrine activity of cysteinyl leukotrienes in human vascular endothelial cells: Signaling through the CysLT₂ receptor.
Published in: Prostaglandins Other Lipid Mediat

Ligand: HAMI3379 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.420000076293945 pIC50
Reference (Journal): Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Published in: Br J Pharmacol

Ligand: HAMI3379 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Published in: Br J Pharmacol

Ligand: compound 15b [PMID: 31811124] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.210000038146973 pIC50
Reference (Journal): Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.
Published in: Nat Commun

Ligand: compound 13e [PMID: 31811124] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pIC50
Reference (Journal): Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.
Published in: Nat Commun

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKB
Reference (Journal): A second cysteinyl leukotriene receptor in human lung.
Published in: J Pharmacol Exp Ther

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene 2 receptor.
Published in: J Biol Chem

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Published in: Br J Pharmacol

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pA2
Reference (Journal): BAYu9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes.
Published in: Eur J Pharmacol

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.16 pEC50
Reference (Journal): Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Published in: Br J Pharmacol

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.52 pIC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor.
Published in: Br J Pharmacol

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.34 pIC50
Reference (Journal): A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice.
Published in: J Pharmacol Exp Ther

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: BAYu9773 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.04 pEC50
Reference (Journal): Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist.
Published in: Mol Pharmacol

Ligand: BayCysLT2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pA2
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J

Ligand: BayCysLT2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pA2
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J

Ligand: BayCysLT2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice.
Published in: J Pharmacol Exp Ther