Target family: Leukotriene receptors (type: gpcr)
Target: CysLT<sub>1</sub> receptor

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma.
Published in: Biochem Pharmacol

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 7.699999809265137 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: yes
Median affinity:  pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 9.59000015258789 pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: zafirlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.
Published in: Br J Pharmacol

Ligand: verlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.96999979019165 pIC50
Reference (Journal): Pharmacology of the leukotriene antagonist verlukast: the (R)-enantiomer of MK-571.
Published in: Can J Physiol Pharmacol

Ligand: verlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Pharmacology of the leukotriene antagonist verlukast: the (R)-enantiomer of MK-571.
Published in: Can J Physiol Pharmacol

Ligand: triple modulator 10 [PMID: 29878767] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pA2
Reference (Journal): Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
Published in: J Med Chem

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 CysLT1 receptor.
Published in: Nature

Ligand: [3H]LTD4 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKd

Ligand: [3H]LTD4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): CysLT1 receptor is a target for extracellular nucleotide-induced heterologous desensitization: a possible feedback mechanism in inflammation.
Published in: J Cell Sci

Ligand: [3H]LTD4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.
Published in: Br J Pharmacol

Ligand: [3H]LTD4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Involvement of prenylated proteins in calcium signaling induced by LTD4 in differentiated U937 cells.
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): 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
Primary target: no
Median affinity: 10.600000381469727 pKd
Reference (Journal): Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.
Published in: Biochem Pharmacol

Ligand: sulukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi

Ligand: SR2640 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma.
Published in: Biochem Pharmacol

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 10 pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: pranlukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.
Published in: Br J Pharmacol

Ligand: pobilukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: pobilukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.260000228881836 pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: pobilukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 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: N-methyl LTC4 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.7 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: montelukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity: 8.550000190734863 pKi
Reference (Journal): Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma.
Published in: Biochem Pharmacol

Ligand: montelukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: montelukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity: 8.640000343322754 pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: montelukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: MK-571 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.41 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:  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:  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): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: LTE4 (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.67 pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

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:  pEC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.05 pIC50
Reference (Journal): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.47 pEC50
Reference (Journal): Involvement of prenylated proteins in calcium signaling induced by LTD4 in differentiated U937 cells.
Published in: Prostaglandins Other Lipid Mediat

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: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): A functional G300S variant of the cysteinyl leukotriene 1 receptor is associated with atopy in a Tristan da Cunha isolate.
Published in: Pharmacogenet Genomics

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:  pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: LTD4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.52 pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

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
Median affinity:  pIC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.68 pEC50
Reference (Journal): Characterization of the human cysteinyl leukotriene CysLT1 receptor.
Published in: Nature

Ligand: LTC4 (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: 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): Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
Published in: Mol Pharmacol

Ligand: iralukast (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.
Published in: Br J Pharmacol

Ligand: ICI198615 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
Published in: J Med Chem

Ligand: compound 15b [PMID: 31811124] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 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: 9 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: 5.3 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: 6.36 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: BayCysLT2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pA2
Reference (Journal): Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor.
Published in: FASEB J