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mf63 compound

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Description

MF63 compound: a phenanthrene imidazole identified as a potent, selective, and orally active mPGES-1 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16070041
CHEMBL ID412099
SCHEMBL ID1758220
MeSH IDM0518620

Synonyms (33)

Synonym
HY-13283
mf63 compound
mf63
mf-63
bdbm50227631
2-(6-chloro-1h-phenanthro[9,10-d]imidazol-2-yl)isophthalonitrile
CHEMBL412099 ,
892549-43-8
CS-0508
1,3-benzenedicarbonitrile, 2-(6-chloro-1h-phenanthro(9,10-d)imidazol-2-yl)-
1,3-benzenedicarbonitrile, 2-(9-chloro-1h-phenanthro(9,10-d)imidazol-2-yl)-
7TU641M876 ,
unii-7tu641m876
mf 63
SCHEMBL1758220
BVFLHOOKHPFDCT-UHFFFAOYSA-N
2-(9-chloro-1h-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
4dz ,
FT-0699579
DTXSID50581753
AKOS030526969
NCGC00485909-01
A916743
BCP21070
mf63; mf 63
2-(6-chloro-3h-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
2-(6-chloro-1h-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile
HMS3740M07
EX-A1887
Q27268842
F84274
MS-26189
AC-36233

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In vivo PK studies in dogs demonstrate 55% oral bioavailability and an 7 h half-life."( Novel benzoxazole inhibitors of mPGES-1.
Berlioz, F; Demian, D; Hoffmaster, K; Kablaoui, N; Moore, WM; Nugent, RA; Patel, S; Shao, J; Vazquez, ML, 2013
)
0.39
" Omission of a lipophilic portion of the compound led to 26, a readily orally bioavailable inhibitor with potency in HWB comparable to celecoxib."( Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
Antonysamy, S; Bhattachar, SN; Campanale, KM; Chandrasekhar, S; Condon, B; Desai, PV; Fisher, MJ; Groshong, C; Harvey, A; Hickey, MJ; Hughes, NE; Jones, SA; Kim, EJ; Kuklish, SL; Luz, JG; Norman, BH; Rathmell, RE; Rizzo, JR; Schiffler, MA; Seng, TW; Thibodeaux, SJ; Woods, TA; York, JS; Yu, XP, 2016
)
0.43
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" It exhibited a significant analgesic effect in a guinea pig hyperalgesia model when orally dosed at 30 and 100mg/kg."( Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Boulet, L; Brideau, C; Claveau, D; Côté, B; Ducharme, Y; Ethier, D; Frenette, R; Friesen, RW; Gagnon, M; Giroux, A; Guay, J; Guiral, S; Mancini, J; Martins, E; Massé, F; Méthot, N; Riendeau, D; Rubin, J; Xu, D; Yu, H, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin E synthaseHomo sapiens (human)IC50 (µMol)0.20060.00102.030810.0000AID1152198; AID1226827; AID1226828; AID1274611; AID1274612; AID1333646; AID1333647; AID1367396; AID1474675; AID1474676; AID446412; AID446413; AID465968; AID580217; AID580218; AID639314; AID698649; AID721277; AID733351
Tyrosine-protein kinase JAK2Homo sapiens (human)IC50 (µMol)0.10000.00010.372210.0000AID317363
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)0.00190.00011.774010.0000AID1333646
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)0.00190.00002.800510.0000AID1333646
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)3.00000.00091.230410.0000AID317360; AID446421
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.00190.00002.398310.0000AID1474675
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC50 (µMol)50.00000.05002.207010.0000AID580219
Tyrosine-protein kinase JAK3Homo sapiens (human)IC50 (µMol)10.00000.00010.41937.9200AID317364
Glutathione transferase Sus scrofa (pig)IC50 (µMol)0.00090.00090.00090.0009AID405542
Prostaglandin E synthase 2Homo sapiens (human)IC50 (µMol)30.00001.60002.10002.6000AID317359; AID446420
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (185)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processProstaglandin E synthaseHomo sapiens (human)
prostaglandin metabolic processProstaglandin E synthaseHomo sapiens (human)
signal transductionProstaglandin E synthaseHomo sapiens (human)
cell population proliferationProstaglandin E synthaseHomo sapiens (human)
negative regulation of cell population proliferationProstaglandin E synthaseHomo sapiens (human)
sensory perception of painProstaglandin E synthaseHomo sapiens (human)
regulation of fever generationProstaglandin E synthaseHomo sapiens (human)
positive regulation of prostaglandin secretionProstaglandin E synthaseHomo sapiens (human)
regulation of inflammatory responseProstaglandin E synthaseHomo sapiens (human)
cellular oxidant detoxificationProstaglandin E synthaseHomo sapiens (human)
positive regulation of platelet aggregationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of platelet activationTyrosine-protein kinase JAK2Homo sapiens (human)
response to antibioticTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of SMAD protein signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
microglial cell activationTyrosine-protein kinase JAK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
chromatin remodelingTyrosine-protein kinase JAK2Homo sapiens (human)
transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
G protein-coupled receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
mesoderm developmentTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell population proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell-substrate adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
response to amineTyrosine-protein kinase JAK2Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase JAK2Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
erythrocyte differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell migrationTyrosine-protein kinase JAK2Homo sapiens (human)
axon regenerationTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular mineralocorticoid receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of insulin secretionTyrosine-protein kinase JAK2Homo sapiens (human)
response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-1 beta productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-17 productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tumor necrosis factor productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of natural killer cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to hydroperoxideTyrosine-protein kinase JAK2Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
symbiont-induced defense-related programmed cell deathTyrosine-protein kinase JAK2Homo sapiens (human)
response to tumor necrosis factorTyrosine-protein kinase JAK2Homo sapiens (human)
post-embryonic hemopoiesisTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to interleukin-3Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-5-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
collagen-activated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-3-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte-macrophage colony-stimulating factor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of protein import into nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
activation of Janus kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of DNA bindingTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MAPK cascadeTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
post-translational protein modificationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MHC class II biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of inflammatory responseTyrosine-protein kinase JAK2Homo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of NK T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
mammary gland epithelium developmentTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of leukocyte proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to interleukin-12Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-35-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to dexamethasone stimulusTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cold-induced thermogenesisTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth factor dependent skeletal muscle satellite cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of epithelial cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of postsynapse to nucleus signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of signaling receptor activityTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
G protein-coupled receptor signaling pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
response to nutrientAldo-keto reductase family 1 member C3Homo sapiens (human)
steroid metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of cell population proliferationAldo-keto reductase family 1 member C3Homo sapiens (human)
male gonad developmentAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to starvationAldo-keto reductase family 1 member C3Homo sapiens (human)
farnesol catabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
cyclooxygenase pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
keratinocyte differentiationAldo-keto reductase family 1 member C3Homo sapiens (human)
progesterone metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
retinal metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
macromolecule metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
regulation of retinoic acid receptor signaling pathwayAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
renal absorptionAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to calcium ionAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to prostaglandin stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to corticosteroid stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to jasmonic acid stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
cellular response to prostaglandin D stimulusAldo-keto reductase family 1 member C3Homo sapiens (human)
negative regulation of retinoic acid biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
regulation of testosterone biosynthetic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of endothelial cell apoptotic processAldo-keto reductase family 1 member C3Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAldo-keto reductase family 1 member C3Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of dendritic cell cytokine productionTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK3Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
B cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-10 productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-12 productionTyrosine-protein kinase JAK3Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
T cell homeostasisTyrosine-protein kinase JAK3Homo sapiens (human)
innate immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of FasL productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T-helper 1 cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T cell activationTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of T cell apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of thymocyte apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-2Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-4Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-15Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-9Tyrosine-protein kinase JAK3Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
lipid metabolic processProstaglandin E synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin E synthase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionProstaglandin E synthase 2Homo sapiens (human)
secretionProstaglandin E synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (75)

Processvia Protein(s)Taxonomy
glutathione transferase activityProstaglandin E synthaseHomo sapiens (human)
glutathione peroxidase activityProstaglandin E synthaseHomo sapiens (human)
prostaglandin-D synthase activityProstaglandin E synthaseHomo sapiens (human)
protein bindingProstaglandin E synthaseHomo sapiens (human)
glutathione bindingProstaglandin E synthaseHomo sapiens (human)
prostaglandin-E synthase activityProstaglandin E synthaseHomo sapiens (human)
protein kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
signaling receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
heme bindingTyrosine-protein kinase JAK2Homo sapiens (human)
type 1 angiotensin receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
acetylcholine receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone H3Y41 kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone bindingTyrosine-protein kinase JAK2Homo sapiens (human)
identical protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
insulin receptor substrate bindingTyrosine-protein kinase JAK2Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK2Homo sapiens (human)
peptide hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityAldo-keto reductase family 1 member C3Homo sapiens (human)
all-trans-retinol dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
oxidoreductase activity, acting on NAD(P)H, quinone or similar compound as acceptorAldo-keto reductase family 1 member C3Homo sapiens (human)
phenanthrene 9,10-monooxygenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
dihydrotestosterone 17-beta-dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin D2 11-ketoreductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
geranylgeranyl reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
ketoreductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
prostaglandin-F synthase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
15-hydroxyprostaglandin-D dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
androsterone dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone dehydrogenase (NAD+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
androstan-3-alpha,17-beta-diol dehydrogenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
ketosteroid monooxygenase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
Delta4-3-oxosteroid 5beta-reductase activityAldo-keto reductase family 1 member C3Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member C3Homo sapiens (human)
bile acid bindingAldo-keto reductase family 1 member C3Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK3Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK3Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
DNA bindingProstaglandin E synthase 2Homo sapiens (human)
protein bindingProstaglandin E synthase 2Homo sapiens (human)
lyase activityProstaglandin E synthase 2Homo sapiens (human)
heme bindingProstaglandin E synthase 2Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityProstaglandin E synthase 2Homo sapiens (human)
glutathione bindingProstaglandin E synthase 2Homo sapiens (human)
prostaglandin-E synthase activityProstaglandin E synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
nuclear envelope lumenProstaglandin E synthaseHomo sapiens (human)
endoplasmic reticulum membraneProstaglandin E synthaseHomo sapiens (human)
membraneProstaglandin E synthaseHomo sapiens (human)
perinuclear region of cytoplasmProstaglandin E synthaseHomo sapiens (human)
membraneProstaglandin E synthaseHomo sapiens (human)
extrinsic component of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
nucleoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK2Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
caveolaTyrosine-protein kinase JAK2Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte macrophage colony-stimulating factor receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
endosome lumenTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
membrane raftTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-23 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
postsynapseTyrosine-protein kinase JAK2Homo sapiens (human)
glutamatergic synapseTyrosine-protein kinase JAK2Homo sapiens (human)
euchromatinTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
nucleusAldo-keto reductase family 1 member C3Homo sapiens (human)
cytoplasmAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C3Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member C3Homo sapiens (human)
cytosolAldo-keto reductase family 1 member C3Homo sapiens (human)
extrinsic component of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
endosomeTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK3Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
Golgi membraneProstaglandin E synthase 2Homo sapiens (human)
extracellular regionProstaglandin E synthase 2Homo sapiens (human)
nucleusProstaglandin E synthase 2Homo sapiens (human)
mitochondrionProstaglandin E synthase 2Homo sapiens (human)
cytosolProstaglandin E synthase 2Homo sapiens (human)
azurophil granule lumenProstaglandin E synthase 2Homo sapiens (human)
perinuclear region of cytoplasmProstaglandin E synthase 2Homo sapiens (human)
mitochondrionProstaglandin E synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (72)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1274617Time-dependent inhibition of microsomal CYP3A4 (unknown origin) using midazolam as substrate assessed as alpha-hydroxymidazolam-d4 at 10 uM pre-incubated for 12 mins before NADPH addition formation after 30 mins by LC-MS/MS analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID405537Inhibition of PGE2 synthesis in human A549 cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID405545Inhibition of PGF2 production in humanixed knock-in mouse stomach at 100 mg/kg2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID446424Analgesic activity against LPS-induced thermal hyperalgesia in po dosed Hartley guinea pig assessed as decrease in paw withdrawal latency administered 1 hr before LPS challenge measured after 4.5 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID580217Inhibition of mPGES12011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.
AID446421Inhibition of TX synthase2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID580219Inhibition of PGF synthase in IL1-beta treated human A549 cell microsome assessed as inhibition of PGF2alpha production after 1 min in presence of 50% FBS2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.
AID1333646Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH
AID405526Inhibition of rat mPGES12008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID446419Inhibition of PGES1 in guinea pig whole blood2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID580220Inhibition of mPGES1 in LPS-stimulated human whole blood assessed as inhibition of PGE2 production2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.
AID1274613Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID317366Cmax in rat at 20 mg/kg, po2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID446417Metabolic stability in rat liver hepatocytes assessed as compound remaining after 2 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID405542Inhibition of guinea pig mPGES12008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID446428Half life in monkey2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID446414Inhibition of PGE2 production in LPS-stimulated human whole blood2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID405539Selectivity for human mPGES1 over PGE22008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID1226828Inhibition of purified mPGES-1 (1 to 152) (unknown origin) extracted from detergent-solubilized baculovirus-infected insect Sf9 cell membranes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.
AID317359Inhibition of human mPGES22007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID1166435Inhibition of guinea pig recombinant mPGES-12014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E(2) synthase-1 inhibitors.
AID405541Inhibition of LPS-stimulated PGE2 production in human whole blood2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID698649Inhibition of mPGES1 expressed in Escherichia coli Rosetta-DE3 assessed as reduction in PGE2 production by enzyme immunoassay based cell-free system assay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.
AID446420Inhibition of human PGES22009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID1152198Inhibition of microsomal PGES-1 (unknown origin) assessed as PGH2 conversion to PGE2 after 1 min by enzyme immunoassay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1.
AID446412Displacement of [3H]PGH2 from human recombinant PGES1 expressed in CHOK1 cells2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID317365Oral bioavailability in rat at 20 mg/kg2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID1333647Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay
AID317358Inhibition of guinea pig mPGES12007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID446413Inhibition of mPGES1 in IL-1-beta-stimulated human A549 cells assessed as blockade of PGH2 to PGE2 conversion in presence of 50% fetal bovine serum2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID405544Inhibition of LPS-induced hyperalgesia in guinea pig2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID317362Inhibition of LPS-stimulated TXB2 production in human whole blood2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID733350Inhibition of PGES-1 in human whole blood assessed as LPS-induced PGE2 formation incubated for 15 mins prior to LPS addition measured after 24 hrs by EIA2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen.
AID446422Inhibition of PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID405538Inhibition of PGE2alpha synthesis in human A549 cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID405546Inhibition of LPS-stimulated TBX2 production in human whole blood2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID721277Inhibition of human recombinant mPGES-1 using PGH2 as substrate incubated 20 mins prior to substrate addition measured after 30 secs by EIA2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Novel benzoxazole inhibitors of mPGES-1.
AID1474675Inhibition of recombinant human mPGES-1 expressed in CHO cells assessed as reduction in PGE2 formation using PGH2 a substrate preincubated for 10 mins followed by substrate addition measured after 1 min2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E
AID1274612Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID317363Inhibition of human JAK22007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID317360Inhibition of TX synthase2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID317357Inhibition of rat mPGES12007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID317361Inhibition of LPS-stimulated PGE2 production in human whole blood2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID317351Inhibition of IL-1-beta-stimulated PGE2 production in human A549 cells in presence of 50% fetal bovine serum2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID1274611Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID405540Selectivity for human mPGES1 over PGE2alpha2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID317367Inhibition of LPS-induced hyperalgesia in guinea pig at 30 mg/kg, po relative to control2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID639314Inhibition of microsomal PGES1 transfected in human HEK293 cells assessed as PGE2 production after 60 mins by HTRF assay2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E₂ synthase-1 inhibitors.
AID580218Inhibition of mPGES1 in IL1-beta treated human A549 cell microsome assessed as inhibition of PGE2 production after 1 min in presence of 50% FBS2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.
AID698648Inhibition of mPGES1 in LPS-stimulated human whole blood assessed as reduction in PGE2 production incubated for 24 hrs at 37 degC by enzyme immunoassay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.
AID1367396Inhibition of mPGES1 in human whole blood assessed as inhibition of LPS-induced PGE2 production measured after 20 to 24 hrs2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-1.
AID317354Inhibition of IL-1-beta-stimulated PGF2alpha production in human A549 cells in presence of 50% fetal bovine serum2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID1226827Inhibition of recombinant human mPGES-1 expressed in human 293E cell microsomes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.
AID733351Inhibition of full-length microsomal PGES-1 (unknown origin) expressed in Escherichia coli Rosetta(DE3) using PGH2 as substrate assessed as inhibition of PGH2 conversion to PGE2 incubated 15 mins prior to substrate addition measured after 1 min by EIA2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen.
AID446418Metabolic stability in human liver hepatocytes assessed as compound remaining after 2 hrs2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID580215Inhibition of TX synthase in LPS-stimulated human whole blood assessed as inhibition of TXB2 production2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.
AID465968Inhibition of human mPGES1 assessed as PGE2 level after 41 sec by ELISA2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.
AID446415Half life in rat at 5 mg/kg, iv administered as single dose2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID1474676Inhibition of mPGES-1 in human A549 cells assessed as decrease in IL1beta induced PGE2 release preincubated for 30 mins followed by IL-1beta addition after 16 to 20 hrs by HTRF method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin E
AID1226829Binding affinity to mPGES-1 (unknown origin) assessed as increase in protein aggregation temperature at 0.1 mM by differential static light scattering method2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.
AID405527Inhibition of human recombinant mPGES1 expressed in CHO cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
AID317364Inhibition of human JAK32007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID317350Inhibition of human recombinant mPGES12007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
AID446423Inhibition of TXB2 production in LPS-stimulated human whole blood2009Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
AID1333648Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated followed by LPS stimulation for 20 to 24 hrs
AID1274616Inhibition of microsomal CYP3A4 (unknown origin) using bufuralol/midazolam/diclofinac as substrate assessed as 1-hydroxybufuralol maleate-d9/alpha-hydroxymidazolam-d4/[13C6]-4-hydroxydiclofinac formation at 10 uM pre-incubated for 10 mins before NADPH add2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
AID317368Inhibition of LPS-induced hyperalgesia in guinea pig at 100 mg/kg, po relative to control2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (17.39)29.6817
2010's17 (73.91)24.3611
2020's2 (8.70)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.81

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 Index11.81 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.98 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.81)

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%
Other23 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]