Page last updated: 2024-08-05 15:23:17

leukotriene antagonist

A drug designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.

ChEBI ID: 49159

Members (9)

MemberDefinitionClass
bay u9773A dicarboxylic acid that is that is (7E,9E,11Z,14Z)-icosa-7,9,11,14-tetraenoic acid substituted by a hydroxy group at position 4S and a (4-carboxyphenyl)sulfanediyl group at 5R. It is a dual cysteinyl leukotriene receptor antagonist that acts at the CysLT1 and CysLT2 receptors (IC50 = 0.44 and 0.30 muM, respectively).BAYu9773
cinalukast2,2-Diethylsuccinanilic acid substituted at a meta- position by an (E)-2-(4-cyclobutyl-1,3-thiazol-2-yl)ethenyl group. It selectively antagonizes leukotriene D4 at the cysteinyl leukotriene receptor, in the human airway, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus. It is used in the treatment of asthma.cinalukast
ici 204,219zafirlukast
knipholoneAn anthraquinone that is anthracene-9,10-dione substituted by hydroxy groups at positions 4 and 6, a methyl group at position 2 and a 3-acetyl-2,6-dihydroxy-4-methoxyphenyl group at position 1. It exhibits antioxidant, cytotoxic and antiplasmodial activities.knipholone
l 663536A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at position 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
ly 171883A member of the class of acetophenones that is 1-phenylethanone substituted at position 2 by a hydroxy group, a propyl group at position 3 and a 4-(1H-tetrazol-5-yl)butoxy group at position 4. A leukotriene antagonist, it exhibits anti-asthmatic activity.tomelukast
montelukastmontelukast
ochnaflavoneA biflavonoid with an ether linkage between the B-rings of the apigenin and luteolin subunits. It has been isolated from several members of the Ochnaceae plant family.ochnaflavone
zileutonA member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogen at position 2 is replaced by a 1-[carbamoyl(hydroxy)amino]ethyl group. A selective 5-lipoxygenase inhibitor, it inhibits the formation of leukotrienes LTB4, LTC4, LDT4, and LTE4. It is used for the management of chronic asthma.zileuton

Research

Studies (3,200)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199059 (1.84)18.7374
1990's591 (18.47)18.2507
2000's1,266 (39.56)29.6817
2010's967 (30.22)24.3611
2020's317 (9.91)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials773 (20.87%)5.53%
Reviews381 (10.29%)6.00%
Case Studies200 (5.40%)4.05%
Observational19 (0.51%)0.25%
Other2,330 (62.92%)84.16%

Protein Targets (182)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency19.118012
15-lipoxygenase, partialHomo sapiens (human)Potency26.200012
acetylcholinesteraseHomo sapiens (human)Potency1.737711
activating transcription factor 6Homo sapiens (human)Potency10.682211
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency11.220211
alpha-galactosidaseHomo sapiens (human)Potency7.079511
AR proteinHomo sapiens (human)Potency15.79701015
aryl hydrocarbon receptorHomo sapiens (human)Potency24.600628
Bloom syndrome protein isoform 1Homo sapiens (human)Potency32.464812
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.118712
Cellular tumor antigen p53Homo sapiens (human)Potency33.763426
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency26.053324
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency32.464812
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency39.810711
Chain A, Beta-lactamaseEscherichia coli K-12Potency0.251211
Chain A, HADH2 proteinHomo sapiens (human)Potency13.896423
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency22.334211
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency18.458813
Chain B, HADH2 proteinHomo sapiens (human)Potency13.896423
cytochrome P450 2C9 precursorHomo sapiens (human)Potency12.589311
cytochrome P450 2C9, partialHomo sapiens (human)Potency19.347014
cytochrome P450 2D6Homo sapiens (human)Potency31.105912
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency8.223526
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency5.921825
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency17.427112
DNA polymerase betaHomo sapiens (human)Potency53.176412
DNA polymerase kappa isoform 1Homo sapiens (human)Potency25.905612
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.7715817
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency31.099123
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.350766
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.465614
EWS/FLI fusion proteinHomo sapiens (human)Potency20.562744
farnesoid X nuclear receptorHomo sapiens (human)Potency33.488911
GVesicular stomatitis virusPotency19.347014
GABA theta subunitRattus norvegicus (Norway rat)Potency8.223513
GALC proteinHomo sapiens (human)Potency0.707911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency8.223513
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency8.223513
gemininHomo sapiens (human)Potency18.316823
GLI family zinc finger 3Homo sapiens (human)Potency18.699824
GLS proteinHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency27.207325
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency13.333211
Guanine nucleotide-binding protein GHomo sapiens (human)Potency5.623411
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency22.387211
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency12.589313
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency13.562313
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency89.125111
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency19.347014
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency23.914511
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency19.347018
Integrin alpha-IIbHomo sapiens (human)Potency28.370812
Integrin beta-3Homo sapiens (human)Potency28.370812
Interferon betaHomo sapiens (human)Potency18.452025
lamin isoform A-delta10Homo sapiens (human)Potency5.722012
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency19.122939
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency12.589311
Microtubule-associated protein tauHomo sapiens (human)Potency33.934025
mitogen-activated protein kinase 1Homo sapiens (human)Potency22.983312
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.000012
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency31.798636
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency45.875612
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency16.935327
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency15.848911
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency19.5546312
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency2.031511
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency9.4310413
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency20.312047
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency24.035312
pregnane X nuclear receptorHomo sapiens (human)Potency30.141637
progesterone receptorHomo sapiens (human)Potency28.577612
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency15.848911
RAR-related orphan receptor gammaMus musculus (house mouse)Potency4.919522
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency23.292935
retinoid X nuclear receptor alphaHomo sapiens (human)Potency31.049236
SMAD family member 2Homo sapiens (human)Potency12.812023
SMAD family member 3Homo sapiens (human)Potency12.812023
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency9.449412
survival motor neuron protein isoform dHomo sapiens (human)Potency14.125411
TAR DNA-binding protein 43Homo sapiens (human)Potency35.481311
TDP1 proteinHomo sapiens (human)Potency20.389628
thioredoxin glutathione reductaseSchistosoma mansoniPotency79.432811
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency33.528127
thyroid stimulating hormone receptorHomo sapiens (human)Potency19.952622
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency10.684011
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency0.794311
tyrosine-protein kinase YesHomo sapiens (human)Potency48.731511
USP1 protein, partialHomo sapiens (human)Potency47.876025
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency16.889724
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency36.441314
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency13.333211

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC506.256011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki3.981011
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC5055.000011
Adenosine receptor A3Homo sapiens (human)IC500.898512
Adenosine receptor A3Homo sapiens (human)Ki0.507512
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.689011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.667011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.898512
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.507512
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.898512
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.507512
Alpha-2A adrenergic receptorHomo sapiens (human)IC503.919011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki1.470011
Alpha-2C adrenergic receptorHomo sapiens (human)IC505.279011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.767011
Arachidonate 5-lipoxygenase-activating proteinHomo sapiens (human)IC500.06471414
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
Beta-2 adrenergic receptorHomo sapiens (human)IC503.488011
Beta-2 adrenergic receptorHomo sapiens (human)Ki2.398011
Beta-3 adrenergic receptorHomo sapiens (human)IC504.300011
Beta-3 adrenergic receptorHomo sapiens (human)Ki3.200011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC501.295522
Bile salt export pumpHomo sapiens (human)IC50319.523346
Bile salt export pumpRattus norvegicus (Norway rat)IC50564.400011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5095.900012
Cannabinoid receptor 2Mus musculus (house mouse)IC50100.000011
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)IC500.002011
Cysteinyl leukotriene receptor 1Homo sapiens (human)IC500.0805911
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Ki0.001924
Cysteinyl leukotriene receptor 1Homo sapiens (human)Ki0.150624
Cysteinyl leukotriene receptor 2Homo sapiens (human)IC5012.852856
Cysteinyl leukotriene receptor 2Homo sapiens (human)Ki0.300112
Cytochrome P450 1A2Homo sapiens (human)Ki117.000011
Cytochrome P450 2C8Homo sapiens (human)IC500.700022
Cytochrome P450 2C9 Homo sapiens (human)IC502.257511
Cytochrome P450 2C9 Homo sapiens (human)Ki2.500011
Cytosolic phospholipase A2Homo sapiens (human)IC5092.500022
D(3) dopamine receptorHomo sapiens (human)IC507.747011
D(3) dopamine receptorHomo sapiens (human)Ki2.631011
Delta-type opioid receptorHomo sapiens (human)IC504.795011
Delta-type opioid receptorHomo sapiens (human)Ki1.690011
Epidermal growth factor receptorHomo sapiens (human)IC504.474012
GABA theta subunitRattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.023011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.023011
Group 10 secretory phospholipase A2Homo sapiens (human)IC50100.000011
Leukotriene A-4 hydrolaseHomo sapiens (human)IC50100.000011
Leukotriene B4 receptor 1Homo sapiens (human)IC500.420011
Leukotriene C4 synthaseHomo sapiens (human)IC504.000022
Macrophage-expressed gene 1 proteinHomo sapiens (human)IC502.200011
Mitogen-activated protein kinase 1Homo sapiens (human)IC500.538011
Mitogen-activated protein kinase 14Homo sapiens (human)IC500.604512
Mitogen-activated protein kinase 3 Homo sapiens (human)IC504.376011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC501.300011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC507.600011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5072.550012
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC508.045011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki1.938011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC506.626011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki1.404011
Phospholipase A2Rattus norvegicus (Norway rat)IC50100.000011
Phospholipase A2, membrane associatedHomo sapiens (human)IC503.500011
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC5018.900012
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC504.24898183
Polyunsaturated fatty acid 5-lipoxygenaseMus musculus (house mouse)IC500.190011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC505.74442020
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)IC5055.000011
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC500.400011
Prostaglandin E synthaseHomo sapiens (human)IC502.17493131
Prostaglandin E synthase 2Homo sapiens (human)IC501.600011
Prostaglandin G/H synthase 1Homo sapiens (human)IC5027.000022
Prostaglandin G/H synthase 1Ovis aries (sheep)IC5041.502544
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC5044.000011
Prostaglandin G/H synthase 2Homo sapiens (human)IC5038.115767
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC5044.000011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5021.520022
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5021.520011
Sodium-dependent dopamine transporter Homo sapiens (human)IC502.601011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki2.067011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC502.689011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.667011
Sodium/bile acid cotransporterHomo sapiens (human)IC504.666733
Solute carrier family 22 member 2Homo sapiens (human)IC509.700011
Substance-K receptorHomo sapiens (human)IC503.822011
Substance-K receptorHomo sapiens (human)Ki1.274011
Thromboxane-A synthaseRattus norvegicus (Norway rat)IC5020.000011
Thromboxane-A synthase Homo sapiens (human)IC502.667512
Tumor necrosis factor ligand superfamily member 11Mus musculus (house mouse)IC5020.000011
Tyrosine-protein kinase FynHomo sapiens (human)IC504.702011
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)Ki6.540011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cysteinyl leukotriene receptor 1Homo sapiens (human)EC500.072011
Cysteinyl leukotriene receptor 1Homo sapiens (human)Kd0.000011
Estrogen receptorRattus norvegicus (Norway rat)EC5033.745716
Estrogen receptor betaRattus norvegicus (Norway rat)EC5033.745716
Leukotriene B4 receptor 1Homo sapiens (human)EC500.470011
Leukotriene B4 receptor 2Homo sapiens (human)EC500.470011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5013.727544
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC5058.400011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC502.440011
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)EC500.470011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC5011.220011
streptokinase A precursorStreptococcus pyogenes M1 GASEC5020.832425

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Kb0.180011
Leukotriene C4 synthaseRattus norvegicus (Norway rat)Inhibition0.003011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)Change0.350022
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)ID500.140011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)Inhibition10.017522
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)Change16.000011
Prostaglandin G/H synthase 1 Bos taurus (cattle)ID50750.000011
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)Change16.000011
Prostaglandin G/H synthase 2 Bos taurus (cattle)ID50750.000011