DGIdb - ZAFIRLUKAST Drug Record

ZAFIRLUKAST chembl:CHEMBL603 Approved

Alternate Names:

ICI-204219
ACCOLATE
ZAFIRLUKAST
4-(5-CYCLOPENTYLOXYCARBONYLAMINO-1-METHYL-1H-INDOL-3-YLMETHYL)-3-METHOXY-N-O-TOLYLSULFONYLBENZAMIDE
ICI-204,219
CYCLOPENTYL 3-(2-METHOXY-4-((O-TOLYLSULFONYL)CARBAMOYL)BENZYL)-1-METHYLINDOLE-5-CARBAMATE
ACCOLATE®
ZD9188
chemidplus:107753-78-6
pubchem.compound:5717
chembl:CHEMBL603
drugbank:00549
rxcui:114970

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antiasthmatic agent
Drug Class	anti-asthmatic agents
Year of Approval	1996

(4 More Sources)

Publications:

Cazzola et al., 2000, Lung function improvement in smokers suffering from COPD with zafirlukast, a CysLT(1)-receptor antagonist., Pulm Pharmacol Ther
Heise et al., 2000, Characterization of the human cysteinyl leukotriene 2 receptor., J. Biol. Chem.
O'Byrne, 1997, Leukotrienes in the pathogenesis of asthma., Chest
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Wang et al., 2000, A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization., J. Biol. Chem.
Murata et al., 2002, [Zafirlukast (Accolate): a review of its pharmacological and clinical profile]., Nippon Yakurigaku Zasshi
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Lee HJ et al., 2016, Effects of CYP2C9 genetic polymorphisms on the pharmacokinetics of zafirlukast., Arch Pharm Res

ZAFIRLUKAST CYSLTR1

Interaction Score: 3.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of Interaction against 10nM LTD4 aequorin-based Ca2+ assay in CHO cells

Details of Interaction zafirlukast is only about 100-fold selective for CysLT1

Details of the Assay for Interaction against [3H]LTD4 in human lung parenchyma

PMIDs:
11061985 10851239 9042024 11752352 11006272 11979731

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

ZAFIRLUKAST CYSLTR2

Interaction Score: 0.75

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of Interaction against LTC4 Ca2+ mobilisation assay in HUVEC

Details of Interaction againist [3H]LTD4 in COS-7 cells

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

ZAFIRLUKAST EPHX2

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
ZAFIRLUKAST CYP2C9

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300 27377818

Sources:
DTC PharmGKB
ZAFIRLUKAST KAT2A

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST PPARG

Interaction Score: 0.03

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology
ZAFIRLUKAST MAPK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST POLB

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST USP1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST CYP2C19

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
ZAFIRLUKAST CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
ZAFIRLUKAST CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
ZAFIRLUKAST BAZ2B

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST VDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST GMNN

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZAFIRLUKAST AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: ZAFIRLUKAST
- Version: 01-August-2011
Alternate Names:

ZAFIRLUKAST Primary Drug Name

Drug Info:

Year of Approval 1996

Drug Class anti-asthmatic agents

Publications:
TdgClinicalTrial: ZAFIRLUKAST
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antiasthmatic agent

Drug Class Small Molecule

FDA Approval approved

Publications:
DTC: ZAFIRLUKAST
- Version: 02-September-2020
Alternate Names:

CHEMBL603 ChEMBL Drug ID

Drug Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
PharmGKB: zafirlukast
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Lee HJ et al., 2016, Effects of CYP2C9 genetic polymorphisms on the pharmacokinetics of zafirlukast., Arch Pharm Res
GuideToPharmacology: 178100355
- Version: 29-September-2020
Alternate Names:

ZAFIRLUKAST GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Zafirlukast
- Version: 2020.06.01
Alternate Names:

D05DVP TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL603
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL603
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Details of Interaction	against 10nM LTD<sub>4</sub> aequorin-based Ca<sup>2+</sup> assay in CHO cells
Details of Interaction	zafirlukast is only about 100-fold selective for CysLT<sub>1</sub>
Details of the Assay for Interaction	against [<sup>3</sup>H]LTD<sub>4</sub> in human lung parenchyma

Details of Interaction	against LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVEC
Details of Interaction	againist [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells
Direct Interaction?	False

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

ZAFIRLUKAST Drug Record

ZAFIRLUKAST chembl:CHEMBL603 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

PMIDs: 11061985 10851239 9042024 11752352 11006272 11979731

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Details of Interaction against LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVEC Details of Interaction againist [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300 27377818

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Agonist

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: ZAFIRLUKAST

Alternate Names: ZAFIRLUKAST Primary Drug Name

Drug Info: Year of Approval 1996 Drug Class anti-asthmatic agents

Publications:

TdgClinicalTrial: ZAFIRLUKAST

Alternate Names:

Drug Info: Drug Indications antiasthmatic agent Drug Class Small Molecule FDA Approval approved

Publications:

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
11061985 10851239 9042024 11752352 11006272 11979731

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of Interaction against LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVEC

Details of Interaction againist [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
22931300 27377818

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

ZAFIRLUKAST Primary Drug Name

Drug Info:

Year of Approval 1996

Drug Class anti-asthmatic agents

Drug Info:

Drug Indications antiasthmatic agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL603 ChEMBL Drug ID

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Publications:

Lee HJ et al., 2016, Effects of CYP2C9 genetic polymorphisms on the pharmacokinetics of zafirlukast., Arch Pharm Res

Alternate Names:

ZAFIRLUKAST GuideToPharmacology Ligand Name

Alternate Names:

D05DVP TTD Drug ID