Page last updated: 2024-12-10

1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylthio]imidazole

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylthio]imidazole is a chemical compound with the following structural formula:

* **1-phenyl:** A phenyl group (C6H5) is attached to the nitrogen atom at position 1 of the imidazole ring.
* **2-[[4-(trifluoromethyl)phenyl]methylthio]:** A [4-(trifluoromethyl)phenyl]methylthio group is attached to the nitrogen atom at position 2 of the imidazole ring. This group consists of a 4-(trifluoromethyl)phenyl group (C6H4CF3) linked to a sulfur atom which is then connected to a methylene group (CH2).

This compound, often abbreviated as **PFMI**, is a **selective antagonist of histamine H4 receptors**. This means it binds to and blocks the H4 receptor, preventing histamine from activating it.

**Importance in Research:**

The H4 receptor is a relatively newly discovered G protein-coupled receptor (GPCR) that is involved in various biological processes, including:

* **Immune system modulation:** H4 receptors play a role in inflammatory responses, leukocyte trafficking, and allergic reactions.
* **Central nervous system function:** They are implicated in cognitive function, sleep-wake cycles, and pain perception.
* **Gastrointestinal system:** H4 receptors influence gut motility and inflammation.

**PFMI has been used extensively in research to study the function and role of H4 receptors.** Its selectivity for H4 receptors makes it a valuable tool to:

* **Investigate the role of H4 receptors in disease:** By blocking H4 receptors, PFMI can help researchers understand its involvement in conditions like asthma, rheumatoid arthritis, inflammatory bowel disease, and even cancer.
* **Develop new drugs:** PFMI acts as a lead compound for the development of novel drugs that target H4 receptors for the treatment of various diseases.

**Example:**

PFMI has been used to investigate the role of H4 receptors in allergic responses. Studies have shown that blocking H4 receptors with PFMI can reduce the severity of allergic reactions in animal models, highlighting its potential for treating allergic diseases.

**In summary, 1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylthio]imidazole (PFMI) is a valuable research tool that has shed light on the function and therapeutic potential of H4 receptors. It has contributed significantly to our understanding of these receptors and their role in various disease processes, opening avenues for the development of novel H4 receptor-targeted therapies.**

Cross-References

ID SourceID
PubMed CID3696046
CHEMBL ID1390514
CHEBI ID114906

Synonyms (19)

Synonym
smr000179722
MLS000327069 ,
1-phenyl-2-{[4-(trifluoromethyl)benzyl]sulfanyl}-1h-imidazole
CHEBI:114906
AKOS005089192
1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylsulfanyl]imidazole
HMS2273D05
3R-0242
478040-08-3
1-phenyl-2-({[4-(trifluoromethyl)phenyl]methyl}sulfanyl)-1h-imidazole
cid_3696046
1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylthio]imidazole
1-phenyl-2-[[4-(trifluoromethyl)benzyl]thio]imidazole
bdbm68853
CHEMBL1390514
Q27196749
HY-153930
CS-0867134
h15-lox-2 inhibitor 1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.28180.003245.467312,589.2998AID2517
glp-1 receptor, partialHomo sapiens (human)Potency7.07950.01846.806014.1254AID624417
TDP1 proteinHomo sapiens (human)Potency23.10930.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency6.30960.00527.809829.0929AID588855
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency25.11890.707912.194339.8107AID720542
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency39.81070.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency44.66840.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency56.23410.006026.168889.1251AID540317
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency14.12540.00798.23321,122.0200AID2551
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency15.84890.075215.225339.8107AID485360
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.84890.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.84890.00638.235039.8107AID881
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency28.18381.000010.475628.1838AID1457
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency79.43283.981146.7448112.2020AID720708
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)IC50 (µMol)0.34000.03201.46494.8000AID1766300
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC50 (µMol)100.00000.00011.68479.3200AID1766305
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC50 (µMol)50.00000.04002.099810.0000AID1766303
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)IC50 (µMol)100.00000.10002.452310.0000AID1766304
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)100.00000.00021.557410.0000AID1766307
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)100.00000.00010.995010.0000AID1766308
[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)
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC50 (µMol)300.00000.212522.156283.9400AID434954
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)EC50 (µMol)0.75000.75000.75000.7500AID1766313
[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 lipoxygenase ALOX15BHomo sapiens (human)Kic0.70000.70000.70000.7000AID1766301
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Kiuc1.20001.20001.20001.2000AID1766302
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (136)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
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)
ossificationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
negative regulation of adaptive immune responsePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
phosphatidylethanolamine biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
inflammatory responsePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
positive regulation of cell-substrate adhesionPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
fatty acid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
bone mineralizationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
positive regulation of actin filament polymerizationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
response to endoplasmic reticulum stressPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cellular response to interleukin-13Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
wound healingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
apoptotic cell clearancePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cellular response to calcium ionPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
regulation of engulfment of apoptotic cellPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
leukotriene A4 metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
negative regulation of muscle cell apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
fatty acid oxidationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
unsaturated fatty acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
superoxide anion generationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
establishment of skin barrierPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
negative regulation of platelet aggregationPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
leukotriene A4 metabolic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipoxin B4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX12Homo 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)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
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)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
hepoxilin-epoxide hydrolase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX12Homo 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)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
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)
lipid dropletPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytoplasmic side of plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)
cytoplasmPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
sarcolemmaPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)
sarcolemmaPolyunsaturated fatty acid lipoxygenase ALOX12Homo 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)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1766316Selectivity ratio of IC50 for inhibition of human COX1 to IC50 for inhibition of human 15-LOX-22021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766300Inhibition of human 15-LOX-2 assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766311Pseudo-peroxidase activity in human 15-LOX-2 assessed as redox activity of the compound by measuring degradation of 13-HpODE at 20 uM by UV/Vis pseudo-peroxidase assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766310Selectivity ratio of IC50 for inhibition of human 12-LOX to IC50 for inhibition of human 15-LOX-22021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766302Uncompetitive inhibition of human 15-LOX-2 assessed as equilibrium dissociation constant from secondary site by measuring 15-HpETE by Dixon plots and Dixon replots analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766305Inhibition of human 5-LOX assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766301Competitive inhibition of human 15-LOX-2 assessed as equilibrium dissociation constant from catalytic site by measuring 15-HpETE by Dixon plots and Dixon replots analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766315Selectivity ratio of IC50 for inhibition of human 5-LOX to IC50 for inhibition of human 15-LOX-22021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766308Inhibition of human recombinant COX-2 assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766317Selectivity ratio of IC50 for inhibition of human COX2 to IC50 for inhibition of human 15-LOX-22021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766313Inhibition of human 15-LOX-2 expressed in HEK293T cells assessed as a reduction in 15-HETE production using arachidonic acid as substrate incubated for 20 mins2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766307Inhibition of human recombinant COX-1 assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766306Inhibition of mouse 15-LOX2 assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766309Selectivity ratio of IC50 for inhibition of human 15-LOX-1 to IC50 for inhibition of human 15-LOX-22021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766312Substrate activity at human 15-LOX-2 assessed as chemical reaction by RP-HPLC analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766314Cytotoxicity against human HEK293T cells expressing human 15-LOX-2 at 10 uM measured after 1 hr by cell survival assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766304Inhibition of human 12-LOX assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
AID1766303Inhibition of human 15-LOX-1 assessed as enzymatic rate using arachidonic acid as substrate by UV/Vis spectrophotometric analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's3 (50.00)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.41

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 Index12.41 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]