Page last updated: 2024-11-12

sb-435495

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Description

SB-435495: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10417440
CHEMBL ID10921
SCHEMBL ID3106248
MeSH IDM0445547

Synonyms (14)

Synonym
bdbm50117772
n-(2-diethylamino-ethyl)-2-[2-(4-fluoro-benzylsulfanyl)-5-(1-methyl-1h-pyrazol-4-ylmethyl)-4-oxo-4h-pyrimidin-1-yl]-n-(4''-trifluoromethyl-biphenyl-4-ylmethyl)-acetamide
CHEMBL10921 ,
SCHEMBL3106248
sb-435495
unii-0ort6zxl2x
1(4h)-pyrimidineacetamide, n-(2-(diethylamino)ethyl)-2-(((4-fluorophenyl)methyl)thio)-5-((1-methyl-1h-pyrazol-4-yl)methyl)-4-oxo-n-((4'-(trifluoromethyl)(1,1'-biphenyl)-4-yl)methyl)-
0ORT6ZXL2X ,
304694-39-1
n-(2-(diethylamino)ethyl)-2-(2-((4-fluorobenzyl)thio)-5-((1-methyl-1h-pyrazol-4-yl)methyl)-4-oxopyrimidin-1(4h)-yl)-n-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)acetamide
vgiqusqbxzxbgw-uhfffaoysa-n
CS-0015514
HY-19415
STARBLD0039987
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)100.00000.00011.774010.0000AID47557
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)10.00000.00011.753610.0000AID47562; AID54918
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)37.00000.00002.015110.0000AID47560; AID54596
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)100.00000.00002.800510.0000AID47559
Voltage-dependent L-type calcium channel subunit alpha-1DRattus norvegicus (Norway rat)IC50 (µMol)10.00000.00131.991510.0000AID47562
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)40.00000.00002.398310.0000AID47558
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC50 (µMol)0.00000.00000.38373.9000AID103814; AID159113
Platelet-activating factor acetylhydrolaseHomo sapiens (human)Ki0.00000.00000.00010.0001AID159115
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (51)

Processvia Protein(s)Taxonomy
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)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo 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)
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)
peptide hormone processingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particle remodelingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
lipid oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
plasma lipoprotein particle oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phosphatidylcholine catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor metabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of inflammatory responsePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of monocyte chemotaxisPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (38)

Processvia Protein(s)Taxonomy
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 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo 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 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo 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 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)
1-alkyl-2-acetylglycerophosphocholine esterase activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phospholipid bindingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
hydrolase activity, acting on ester bondsPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
calcium-independent phospholipase A2 activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo 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 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)
extracellular regionPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
high-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID47558Inhibition of cytochrome P450 2C192002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID159112Inhibition of the Phospholipase A2 (Lp-PLA2) enzyme in whole human plasma2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID47562Inhibition of cytochrome P450 3A42002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID47559Inhibition of cytochrome P450 2C92002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID88966Concentration required to inhibit the production of lyso-PtdCho by the compound during the copper catalyzed oxidation of human LDL2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID159116Binding against Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) in WHHL rabbit plasma (100 nM)2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID47560Inhibition of cytochrome P450 2D62002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID103814Inhibitory activity against recombinant human Lp-PLA22003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID21272Permeability of compound was evaluated in an artificial membrane permeability assay2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID159114Binding against Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) in whole human plasma (10 nM)2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID13394Oral bioavailability in fed rat2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID21273Permeability was determined2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID103966Non specific binding effect against Lp-PLA2 was determined in rabbit plasma at 100 nM2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID159113Inhibitory concentration against Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) was estimated2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID54596Inhibitory activity against Cytochrome P450 2D62003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID9316Oral bioavailability in dog2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID8503Oral bioavailability in dog2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID54918Inhibitory activity against CYP450 3A4 isozyme2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID21738Solubility in pure water at pH 4.72002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID159115Steady state and transient kinetics to a freely reversible, non-covalently bound, human recombinant Phospholipase A2 (rhLp-PLA2) was determined2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID13329Oral bioavailability in rat2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID103822Non specific binding effect against Lp-PLA2 was determined in human plasma at 10 nM2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID159117Inhibitory concentration against Lp-PLA2 was estimated 2 hr after administration of 30 mg/Kg in WHHL rabbit2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID47557Inhibition of cytochrome P450 1A22002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
AID13393Oral bioavailability in fasted rat2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
AID88967Concentration required to inhibit the subsequent monocyte chemotaxis by the compound during the copper catalyzed oxidation of human LDL2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (60.00)29.6817
2010's2 (40.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.63

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

MetricThis Compound (vs All)
Research Demand Index12.63 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.63)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]