Page last updated: 2024-11-06

bw-755c

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Description

4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine: A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID47795
CHEMBL ID274642
SCHEMBL ID2573191
MeSH IDM0024166

Synonyms (38)

Synonym
bw-755c
66000-40-6
4,5-dihydro-1-(3-(trifluoromethyl)phenyl)-1h-pyrazol-3-amine
1h-pyrazol-3-amine, 4,5-dihydro-1-(3-(trifluoromethyl)phenyl)-
bw 755c
bw755c
CHEMBL274642 ,
2-[3-(trifluoromethyl)phenyl]-3,4-dihydropyrazol-5-amine
bdbm50000540
1-(3-trifluoromethylphenyl)-4,5-dihydro-1h-3-pyrazolamine
1-(3-trifluoromethyl-phenyl)-4,5-dihydro-1h-pyrazol-3-ylamine (bw-755c)
1-(3-trifluoromethyl-phenyl)-4,5-dihydro-1h-pyrazol-3-ylamine(bw 755c)
1-(3-trifluoromethyl-phenyl)-4,5-dihydro-1h-pyrazol-3-ylamine
1-(3-trifluoromethyl-phenyl)-4,5-dihydro-1h-pyrazol-3-ylamine(bw 755 c)
AKOS001035530
unii-6v6jf56bxo
6v6jf56bxo ,
einecs 266-051-8
1-(3-trifluoromethylphenyl)-4,5-dihydro-1h-pyrazol-3-amine
3-amino-1-(3-trifluoromethylphenyl)-2-pyrazoline
3-amino-1-(alpha,alpha,alpha-trifluoro-m-tolyl)-2-pyrazoline
1-[3-(trifluoromethyl)phenyl]-3-amino-2-pyrazoline
1-[3-(trifluoromethyl)phenyl]-4,5-dihydro-1h-pyrazol-3-amine
SCHEMBL2573191
3-amino-1-(m-(trifluoromethyl)phenyl)-2-pyrazoline
amino-1-(3-(trifluoromethyl)phenyl)-2-pyrazoline, 3-
3-amino-1-(3-(trifluoromethyl)phenyl)-2-pyrazoline
3-amino-1-(3-(trifluoromethyl)phenyl)pyrazoline
compound bw 755c
DTXSID30216213
sr-01000025386
SR-01000025386-1
Z56758476
1-(3-(trifluoromethyl)phenyl)-4,5-dihydro-1h-pyrazol-3-amine
Q27265569
CS-0077798
EN300-172424
HY-119671

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Bioavailability and selectivity were assessed by ex vivo RIA of TXB2, LTB4, and 12-HETE from ionophore-challenged blood."( Simple procedure for measuring the pharmacodynamics and analgesic potential of lipoxygenase inhibitors.
Carey, F; Edmonds, AE; Forder, RA; Haworth, D, 1988
)
0.27

Dosage Studied

ExcerptRelevanceReference
" Neither indomethacin (1 mumol/L) nor the cyclo-oxygenase/lipoxygenase inhibitor BW755C (1 mumol/L) had any significant effect on the log dose-response curve to ET-1 in either group of kidneys."( Increased sensitivity to endothelin-1 in isolated Krebs'-perfused kidneys of streptozotocin-diabetic rats.
Hodgson, WC; King, RG; Tammesild, PJ, 1992
)
0.28
" TNF alpha potentiated the release of [3H]arachidonate and PRL promoted by phospholipase-A2 and melittin, and markedly shifted the dose-response curve to the left."( Tumor necrosis factor-alpha increases release of arachidonate and prolactin from rat anterior pituitary cells.
Hirota, K; Ikegami, H; Kadowaki, K; Koike, K; Miyake, A; Ohmichi, M; Tanizawa, O; Yamaguchi, M, 1991
)
0.28
" Airway responsiveness was assessed with dose-response curves of acetylcholine aerosol versus pulmonary resistance in two sets of experiments."( An anti-inflammatory drug (BW755C) inhibits airway hyperresponsiveness induced by ozone in dogs.
Aizawa, H; Bethel, RA; Fabbri, LM; Holtzman, MJ; Nadel, JA; O'Byrne, PM; Walters, EH, 1985
)
0.27
" Inhibition of LTB4-formation and cell migration by BW755C was dose-related, but the two dose-response curves were not parallel."( The effects of BW755C and other anti-inflammatory drugs on eicosanoid concentrations and leukocyte accumulation in experimentally-induced acute inflammation.
Moncada, S; Salmon, JA; Simmons, PM, 1983
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC50 (µMol)3.00000.00011.68479.3200AID6733
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)5.23900.00462.018210.0000AID179757; AID3633; AID6809; AID6829; AID6849; AID6855; AID6870; AID7057; AID7079; AID7096
Cytochrome P450 11B1, mitochondrialRattus norvegicus (Norway rat)IC50 (µMol)5.00000.49503.52895.0000AID179759
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)12.00000.00021.557410.0000AID160848
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00132.22068.3000AID179759
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00321.79008.3000AID179759
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC50 (µMol)5.00000.00321.54318.3000AID179759
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)12.00000.00010.995010.0000AID160848
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)5.50000.00291.786810.0000AID161024; AID179759
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC50 (µMol)5.00000.00321.54318.3000AID179759
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)5.50000.00291.823210.0000AID161024; AID179759
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)EC50 (µMol)6.80000.07002.86006.8000AID101298
Leukotriene B4 receptor 1Homo sapiens (human)EC50 (µMol)6.80000.07002.44676.8000AID101298
Leukotriene B4 receptor 2Homo sapiens (human)EC50 (µMol)6.80000.07001.93756.8000AID101298
[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)Change10.50000.30003.566710.0000AID6772; AID6773
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)Change6.00000.10002.60008.0000AID160867; AID160868
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)Change6.00000.10002.60008.0000AID160867; AID160868
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (99)

Processvia Protein(s)Taxonomy
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
muscle contractionLeukotriene B4 receptor 1Homo sapiens (human)
inflammatory responseLeukotriene B4 receptor 1Homo sapiens (human)
immune responseLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
chemotaxisLeukotriene B4 receptor 2Homo sapiens (human)
negative regulation of adenylate cyclase activityLeukotriene B4 receptor 2Homo sapiens (human)
keratinocyte migrationLeukotriene B4 receptor 2Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
nucleotide bindingLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
nucleoplasmLeukotriene B4 receptor 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 2Homo sapiens (human)
membraneLeukotriene B4 receptor 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
AID160716Inhibition of Prostaglandin G/H synthase from bovine seminal vesicle at 20 uM concentration1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
AID226136Antiinflammatory activity was assessed by the ability to improve the adjuvant induced arthritis in right secondary lesion in rats (volume change in the injected paw measured from day 9 to day 18); ND = no data1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID161024In vitro for prostaglandin G/H synthase inhibitory activity against rat basophil leukemia type 1 cell homogenates, by measuring the radioactivity of [14C]-PGD21990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
AID6855In vitro inhibition of 5-lipoxygenase in rat (peritoneal assay)1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
AID76638Compound was evaluated for the inhibition of leukotriene-mediated bronchoconstriction in guinea pig (in vivo)1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones.
AID67735-lipoxygenase inhibitory activity against rat polymorphonuclear leucocytes from female wistar rat, by using LTB4.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
AID160868Inhibition of prostaglandin G/H synthase pathway in rat polymorphonuclear assay by ability to inhibit formation of TXB2 at 10 uM.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
AID77212Tested for effect on the production of Lipoxygenase (LOX) metabolite, 5-HETE in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID179759In vitro inhibition of PGE-2 production was measured in rat blood1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID160848The compound was tested for inhibitory activity against Prostaglandin G/H synthase in human 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.
AID226134Antiinflammatory activity was assessed by the ability to improve the adjuvant induced arthritis in left secondary lesion in rats ( volume change in the injected paw measured from day 9 to day 18); ND = no data1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID67725-lipoxygenase inhibitory activity against rat polymorphonuclear leucocytes from female wistar rat, by using 5-HETE.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
AID77214Tested for effect on the production of cyclooxygenase (COX) metabolite, PGE-2 (prostaglandin E2) of arachidonic acid in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID77218Tested for effect on the production of cyclooxygenase (COX) metabolite, PGF2-alpha (prostaglandin F2-alpha) of arachidonic acid in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID171862Anti-inflammatory activity by rat carrageenan edema assay. (3h edema).1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
AID93590In vitro methemoglobin Induction at 10e-4 M in lysed human red blood cells1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
AID132112In vivo inhibition of ear oedema in mice following p.o. administration.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
AID77221Tested for effect on the production of cyclooxygenase (COX) metabolite, TXB2 of arachidonic acid in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID162159Inhibitory activity against Prostaglandin G/H synthase 1 isolated from ram (sheep) seminal vesicle at 300 uM concentration; NT=not tested1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
AID184031In vivo activity against the release of SRS(slow releasing substance)-A in a rat passive intraperitoneally1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Novel 1H-benzimidazol-4-ols with potent 5-lipoxygenase inhibitory activity.
AID7096In vitro inhibition of 5-lipoxygenase (5-lo) from the 20000 g supernatant of RBI-1 cells1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
4-hydroxythiazole inhibitors of 5-lipoxygenase.
AID160739Inhibitory activity against Prostaglandin G/H synthase 2 obtained from sheep placenta at 300 uM concentration; NT=not tested1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
AID132224In vivo inhibition of AA induced ear oedema in mice following topical administration.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
AID77206Tested for effect on the production of Lipoxygenase (LO) metabolite, 5,12-diHETE in guinea pig peritoneal polymorphonuclear neutrophils at 30 uM concentration1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID6733The compound was tested for inhibitory activity against 5-lipoxygenase in human 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.
AID226135Antiinflammatory activity was assessed by the ability to improve the adjuvant induced arthritis in right primary lesion in rats (volume change in the injected paw measured from day 0 to day 8); ND = no data1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
5-Acyl-3-substituted-benzofuran-2(3H)-ones as potential antiinflammatory agents.
AID3633In vitro inhibition of rat 5-Lipoxygenase1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones.
AID179757In vitro inhibition of LTB4 production was measured in rat blood1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
AID101295Ex vivo inhibition of LTB4 production was measured in dog blood1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
AID3647Compound was evaluated for the inhibition of 5-Lipoxygenase (5-LO) ex vivo1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones.
AID79022Evaluated for inhibition of the formation and release of SRS-A in isolated guinea pig ileum1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Studies on hindered phenols and analogues. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity.
AID7057Inhibitory activity against 5-lipoxygenase obtained from rat basophilic leukemia cells1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
AID6829In vitro inhibition of RBL-1 5-lipoxygenase; Value ranges from 0.72-1.071987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Novel 1H-benzimidazol-4-ols with potent 5-lipoxygenase inhibitory activity.
AID102477Inhibitory activity against Leukotriene B4 receptor in human PMN1992Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7
Development of 2,3-dihydro-6-(3-phenoxypropyl)-2-(2-phenylethyl)-5-benzofuranol (L-670,630) as a potent and orally active inhibitor of 5-lipoxygenase.
AID7079Iin vitro inhibition of 5-lipoxygenase activity in rat basophil leukemia type 1(RBL1) cell homogenates, (reduction of [14C]-5-HETE formation)1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
AID76098Inhibition of CCl4 induced lipid peroxidation (LPO) of guinea pig hepatic microsomes at 300 uM concentration; NT=not tested1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
AID6968Evaluated for inhibition of the formation and release of 5-lipoxygenase in isolated guinea pig ileum1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Studies on hindered phenols and analogues. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity.
AID104159Inhibitory activity against lipoxygenase (LO) at 10 uM concentration1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Antiinflammatory 2,6-di-tert-butyl-4-(2-arylethenyl)phenols.
AID171859Anti-inflammatory activity by rat adjuvant Arthritis assay. (3h edema).1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
AID101298In vitro inhibition of ionophore stimulated LTB4 release from human peripheral blood leukocytes.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.
AID6809In vitro inhibitory activity against RBL-1 5-LO1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Hydroxamic acid inhibitors of 5-lipoxygenase.
AID127801In vivo 5-Lipoxygenase inhibitory activity by using mouse zymosan peritonitis model1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.
AID6870Inhibition of 5-lipoxygenase in rat RBL-1 cells1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
AID160867Inhibition of Prostaglandin G/H synthase pathway in rat polymorphonuclear assay by ability to inhibit formation of PGE-2 at 10 uM1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.
AID6849In vitro inhibitory activity against 5-lipoxygenase from rat basophilic leukemia cells.1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Synthesis and 5-lipoxygenase inhibitory activity of 5-hydroperoxy-6,8,11,14-eicosatetraenoic acid analogues.
AID493017Wombat Data for BeliefDocking1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (450)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990297 (66.00)18.7374
1990's141 (31.33)18.2507
2000's12 (2.67)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: 7.88

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 Index7.88 (24.57)
Research Supply Index6.14 (2.92)
Research Growth Index4.02 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (7.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (0.65%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other459 (99.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]