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wy 45911

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Description

Wy 45911: a leukotriene antagonist with lipoxygenase inhibiting activity; structure given in UD [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID129110
CHEMBL ID287012
SCHEMBL ID8181188
MeSH IDM0152435

Synonyms (13)

Synonym
wy 45911
CHEMBL287012 ,
wy-45911
n-hydroxy-n-[3-(quinolin-2-ylmethoxy)-phenyl]-succinamic acid methyl ester (wy-45,911)
n-hydroxy-n-[3-(quinolin-2-ylmethoxy)-phenyl]-succinamic acid methyl ester
bdbm50006801
methyl 4-[n-hydroxy-3-(quinolin-2-ylmethoxy)anilino]-4-oxobutanoate
4-(hydroxy-(3-(2-quinolinylnethoxy)phenyl)amino)-4-oxobutanoic acid methyl ester
wy-45,911
butanoic acid, 4-(hydroxy(3-(2-quinolinylmethoxy)phenyl)amino)-4-oxo-, methyl ester
105785-61-3
SCHEMBL8181188
DTXSID60147344
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)1.40000.00462.018210.0000AID104166; AID3639; AID6799; AID6818
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)40.13330.00291.786810.0000AID160873; AID160876; AID220183
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)40.13330.00291.823210.0000AID160873; AID160876; AID220183
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)Inhibition1.53000.03500.78251.5300AID3642
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID192571Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.15 mg per plate, with activation provided by S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID192560Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.005 mg per plate, without activation in the absence of S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID166555The compound was tested for inhibition of translocation in SAR in RBL-2H3 cells1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID78034Compound was evaluated in vivo for the percent inhibition of Ovalbumin-induced (OA) bronchospasm in guinea pig at dose of 50 mg/kg id1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID73693Compound was evaluated for its effect on LTD4-induced contraction of guinea pig trachea1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID76183Ability to inhibit the Ovalbumin induced bronchospasm in guinea pig was determined in vivo at a dose of 50 mg/kg id1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID104166Ability to inhibit Lipoxygenase in vitro was determined1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID77094In vitro LTD4-induced bronchoconstriction. i n isolated guinea pig trachea by injecting intraduodenally.1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID192566Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.05 mg per plate, with activation provided by S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID79843Compound was evaluated for its effect on LTC4-induced contraction of guinea pig trachea1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID224275The compound was tested for inhibition of thromboxane B2 synthesis1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID192567Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.05 mg per plate, without activation in the absence of S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID192562Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.015 mg per plate, without activation in the absence of S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID76181Inhibition of LTB4 induced bronchospasm in guinea pig was determined in at 50 mg/kg i.d.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID3642The compound was tested for inhibition of isolated 5-Lipoxygenase1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID151318In vitro inhibition of ovalbumin-induced bronchoconstriction in isolated guinea pig trachea was determined after intraduodenal aministration1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID73692Compound was evaluated for its effect on LTC4-induced contraction of guinea pig trachea1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID23089-log dissociation constant was determined In vitro in isolated guinea pig trachea after intraduodenal administration (before 10 min)1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID220183Ability to inhibit the rat PMN (polymorphonuclear leukocyte) CO (cyclo-oxygenase) in vitro was determined1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID78031In vivo inhibition of LTD4-induced bronchospasm in guinea pig at dose of 50 mg/kg1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID78083Compound was evaluated for its effect on LTD4-induced contraction of guinea pig trachea; percentage of maximal response of tissue to carbachol1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID224276The compound was tested for inhibitory activity against LTC4 synthesis in mouse peritoneal macrophages1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID192577Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.5 mg per plate, with activation provided by S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID224274The compound was tested for inhibition of prostaglandin E2[PGE2] synthesis1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID79844Compound was evaluated for its effect on LTD4-induced contraction of guinea pig trachea1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID160873In vitro inhibition of rat polymorphonuclear leukocyte (PMN) Prostaglandin G/H synthase1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID3639The compound was tested for inhibitory activity against 5-Lipoxygenase receptor in rat polymorphonuclear leukocytes[PMNS]1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID192695Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.5 mg per plate, without activation in the absence of S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID192572Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.15 mg per plate, without activation in the absence of S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID192561Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.015 mg per plate, with activation provided by S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
AID224396The compound was tested for maximal inhibition against LTC4 synthesis in mouse peritoneal macrophages1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID78081Compound was evaluated for its effect on LTC4-induced contraction of guinea pig trachea; percentage of maximal response of tissue to carbachol1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID6799Inhibition of rat polymorphonuclear leukocyte (PMN) 5-Lipoxygenase in vitro1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
AID6818Concentration that produces 50% inhibition of A-23187-stimulated radiolabeled 5-HETE and TXB2 synthesis by PMN 5-lipoxygenase.1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID166554The compound was tested for inhibition LTC4 synthesis1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID160876Concentration that produces 50% inhibition of A-23187-stimulated radiolabeled 5-HETE and TXB2 synthesis by PMN (Prostaglandin G/H synthase).1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID192559Tested for metabolic activation counted as mean number of revertants in strains TA98, TA100, TA1535, and TA1538, three plates per treatment at 0.005 mg per plate, with activation provided by S-9 rat liver homogenates in Ames test1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (71.43)18.7374
1990's2 (28.57)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.26

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.26 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]