Page last updated: 2024-11-11

s 1360

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Cross-References

ID SourceID
PubMed CID6451047
CHEMBL ID368084
CHEMBL ID218227
SCHEMBL ID10070153
SCHEMBL ID3221454
MeSH IDM0420446

Synonyms (24)

Synonym
gw-810781
gsk-s-1360
280571-30-4
s-1360 ,
2-propen-1-one, 1-[5-[(4-fluorophenyl)methyl]-2-furanyl]-3-hydroxy-3-(1h-1,2,4-triazol-3-yl)-
(z)-1-[5-[(4-fluorophenyl)methyl]-2-furyl]-3-hydroxy-3-(1h-1,2,4-triazol-3-yl)prop-2-en-1-one
1-[5-(4-fluorobenzyl)furan-2-yl]-3-hydroxy-3-(1h-1,2,4-triazol-3-yl)propene
s 1360
gw810781
chembl368084 ,
CHEMBL218227
(z)-1-[5-[(4-fluorophenyl)methyl]furan-2-yl]-3-hydroxy-3-(1h-1,2,4-triazol-5-yl)prop-2-en-1-one
w7kqu075cv ,
2-propen-1-one, 1-(5-((4-fluorophenyl)methyl)-2-furanyl)-3-hydroxy-3-(1h-1,2,4-triazol-3-yl)-
1-(5-(4-fluorobenzyl)furan-2-yl)-3-hydroxy-3-(1h-1,2,4-triazol-3-yl)propene
unii-w7kqu075cv
SCHEMBL10070153
SCHEMBL3221454
(z)-1-(5-((4-fluorophenyl)methyl)-2-furyl)-3-hydroxy-3-(1h-1,2,4-triazol-3-yl)prop-2-en-1-one
2-propen-1-one, 1-(5-((4-fluorophenyl)methyl)-2-furanyl)-3-hydroxy-3-(1h-1,2,4-triazol-5-yl)-
1-(5-(4-fluorobenzyl)furan-2-yl)-3-hydroxy-3-(1h-(1,2,4)triazol-3-yl)propenone
bdbm50476348
2-propen-1-one, 1-[5-[(4-fluorophenyl)methyl]-2-furanyl]-3-hydroxy-3-(1h-1,2,4-triazol-5-yl)-
AKOS040746316
[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)
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)0.02000.00010.995010.0000AID241600
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.02000.00011.076810.0000AID242192
Integrase Human immunodeficiency virus 1IC50 (µMol)3.87330.00051.544310.0000AID241600; AID254835; AID287280; AID287281; AID311010; AID578845; AID578846; AID780331; AID780332
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID578845Inhibition of Human immunodeficiency virus 1 integrase strand transfer activity after 30 mins by polyacrylamide gel electrophoresis2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors.
AID364242Antiviral activity against HIV1 with integrase T66I mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID364245Antiviral activity against HIV1 with integrase T125K mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID364246Antiviral activity against HIV1 with integrase T66I/M154 mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID762839Antiviral activity against HCV infected in human Huh7 cells assessed as inhibition of viral replication by measuring EGFP autofluorescence at 50 uM by CCK8 assay relative to control2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents.
AID364247Antiviral activity against HIV1 with integrase T66I/S153Y mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID289131Antiviral activity against HIV2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
3-Hydroxy-1,5-dihydro-pyrrol-2-one derivatives as advanced inhibitors of HIV integrase.
AID364243Antiviral activity against HIV1 with integrase V151I mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID276001Inhibition of recombinant HIV integrase strand transfer activity2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones.
AID364249Antiviral activity against HIV1 with integrase T125K/F121Y mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID666284Antiviral activity against HIV2011ACS medicinal chemistry letters, Oct-05, Volume: 2, Issue:12
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity.
AID287281Inhibition of HIV1 integrase strand transfer activity2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.
AID364248Antiviral activity against HIV1 with integrase N155S mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID364250Antiviral activity against HIV1 with integrase T66I/L74M/V151I mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID780332Inhibition of Human immunodeficiency virus 1 integrase strand transfer activity after 30 mins by polyacrylamide gel electrophoresis2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors.
AID780331Inhibition of Human immunodeficiency virus 1 integrase-mediated 3'-processing after 30 mins by polyacrylamide gel electrophoresis2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors.
AID666286Therapeutic index, ratio of CC50 for PBMC to EC50 for HIV2011ACS medicinal chemistry letters, Oct-05, Volume: 2, Issue:12
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity.
AID666288Inhibition of HIV integrase-mediated strand transfer2011ACS medicinal chemistry letters, Oct-05, Volume: 2, Issue:12
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity.
AID578846Inhibition of Human immunodeficiency virus 1 integrase-mediated 3'-processing after 30 mins by polyacrylamide gel electrophoresis2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors.
AID666285Cytotoxicity against PBMC2011ACS medicinal chemistry letters, Oct-05, Volume: 2, Issue:12
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity.
AID311010Inhibition of HIV1 integrase2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
Calculation of binding energy using BLYP/MM for the HIV-1 integrase complexed with the S-1360 and two analogues.
AID287280Inhibition of HIV1 integrase 3'-end processing activity2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors.
AID364244Antiviral activity against HIV1 with integrase F121Y mutation by single cycle infectivity assay in presence of 10%FBS2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
AID241600Inhibitory concentration against human immunodeficiency virus type 1 integrase2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
New approaches toward anti-HIV chemotherapy.
AID245897Cytotoxic concentration of the compound to inhibit HIV 1 replication2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
New approaches toward anti-HIV chemotherapy.
AID246213Effective concentration of the compound to inhibit human immunodeficiency virus type 1 replication2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
New approaches toward anti-HIV chemotherapy.
AID242192Concentration required to inhibit catalytic activity of human immuno deficiency virus type 1 integrase2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Beta-diketo acid pharmacophore hypothesis. 1. Discovery of a novel class of HIV-1 integrase inhibitors.
AID254835Strand transfer inhibitory activity against HIV-1 integrase2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's21 (84.00)29.6817
2010's4 (16.00)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: 31.63

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.63 (24.57)
Research Supply Index3.30 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index37.86 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.63)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (15.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (84.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]