Page last updated: 2024-12-11

efipladib

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Description

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

Cross-References

ID SourceID
PubMed CID9853499
CHEMBL ID272342
SCHEMBL ID1500831
MeSH IDM0524384

Synonyms (32)

Synonym
efipladib (usan)
D06674
381683-94-9
bdbm50226792
4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1h-indol-3-yl]propyl}benzoic acid
CHEMBL272342 ,
efipladib
pla-902
s97yug2a91 ,
4-(3-(5-chloro-2-(2-(((3,4-dichlorobenzyl)sulfonyl)amino)ethyl)-1-(diphenylmethyl)-1h-indol-3-yl)propyl)benzoic acid
4-(3-(5-chloro-2-(2-((((3,4-dichlorophenyl)methyl)sulfonyl)amino)ethyl)-1-(diphenylmethyl)-1h-indol-3-yl)propyl)benzoic acid
efipladib [usan:inn]
unii-s97yug2a91
4-[3-[5-chloro-2-[2-[[(3,4-dichlorobenzyl)sulfonyl]amino]ethyl]-1-(diphenylmethyl)-1h-indol-3-yl]propyl]benzoic acid
efipladib [inn]
efipladib [usan]
benzoic acid, 4-(3-(5-chloro-2-(2-((((3,4-dichlorophenyl)methyl)sulfonyl)amino)ethyl)-1-(diphenylmethyl)-1h-indol-3-yl)propyl)-
4-[3-[5-chloro-2-[2-[[[(3,4-dichlorophenyl)-methyl]-su lfonyl]amino]ethyl]-1-(diphenylmethyl)-1h-indol-3-yl]propyl]benzoic acid
4-{3-[1-benzhydryl-5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1h-indol-3-yl]propyl}benzoic acid
4-[3-[5-chloro-2-[2-[[[(3,4-dichlorophenyl)-methyl]-sulfonyl]amino]ethyl]-1-(diphenylmethyl)-1h-indol-3-yl]propyl]benzoic acid
4-(3-{1-benzhydryl-5-chloro-2-[2-(3,4-dichloro-phenylmethanesulfonylamino)-ethyl]-1h-indol-3-yl}-propyl)-benzoic acid
HIZOPJQOPKRKFM-UHFFFAOYSA-N
4-[3-[5-chloro-2-[2-[[[(3,4-dichlorophenyl)-methyl]-sulfonyl]amino]ethyl]-1-(diphenylmethyl)-1h-indol-3-yl]propyl] benzoic acid
SCHEMBL1500831
4-[3-[1-benzhydryl-5-chloro-2-[2-[(3,4-dichlorophenyl)methylsulfonylamino]ethyl]indol-3-yl]propyl]benzoic acid
Q27289073
4-(3-(1-benzhydryl-5-chloro-2-(2-(((3,4-dichlorophenyl)methyl)sulfonamido)ethyl)-1h-indol-3-yl)propyl)benzoic
4-{3-[5-chloro-2-(2-{[(3,4-dichlorophenyl)methanesulfonyl]amino}ethyl)-1-(diphenylmethyl)-1h-indol-3-yl]propyl}benzoic acid
DTXSID20870343
CS-0025432
HY-106253
AKOS040748307

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Finally, these compounds have shown efficacy when dosed orally in multiple acute and chronic prostaglandin and leukotriene dependent in vivo models."( Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
Abraham, WM; Albert, L; Behnke, ML; Chen, L; Clark, JD; Donahue, F; Foley, MA; Goodwin, DG; Hegen, M; Hu, B; Hu, Y; Ipek, M; Keith, J; Kirincich, SJ; Ku, MS; Lee, KL; McKew, JC; Michalak, R; Murphy, EA; Nickerson-Nutter, CL; Ramarao, MK; Shen, MW; Sum, FW; Tam, S; Thakker, P; Thomason, J; Williams, C; Wooder, L; Wu, K; Xu, X, 2008
)
0.53
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytosolic phospholipase A2Homo sapiens (human)IC50 (µMol)0.02030.00051.09862.3000AID1187018; AID345901
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processCytosolic phospholipase A2Homo sapiens (human)
positive regulation of T-helper 1 type immune responseCytosolic phospholipase A2Homo sapiens (human)
glycerol metabolic processCytosolic phospholipase A2Homo sapiens (human)
monoacylglycerol biosynthetic processCytosolic phospholipase A2Homo sapiens (human)
platelet activating factor biosynthetic processCytosolic phospholipase A2Homo sapiens (human)
icosanoid metabolic processCytosolic phospholipase A2Homo sapiens (human)
positive regulation of platelet activationCytosolic phospholipase A2Homo sapiens (human)
arachidonic acid metabolic processCytosolic phospholipase A2Homo sapiens (human)
leukotriene biosynthetic processCytosolic phospholipase A2Homo sapiens (human)
positive regulation of prostaglandin secretionCytosolic phospholipase A2Homo sapiens (human)
phosphatidylglycerol catabolic processCytosolic phospholipase A2Homo sapiens (human)
phosphatidylcholine catabolic processCytosolic phospholipase A2Homo sapiens (human)
phosphatidylcholine acyl-chain remodelingCytosolic phospholipase A2Homo sapiens (human)
regulation of cell population proliferationCytosolic phospholipase A2Homo sapiens (human)
positive regulation of macrophage activationCytosolic phospholipase A2Homo sapiens (human)
arachidonic acid secretionCytosolic phospholipase A2Homo sapiens (human)
establishment of localization in cellCytosolic phospholipase A2Homo sapiens (human)
cellular response to antibioticCytosolic phospholipase A2Homo sapiens (human)
glycerophospholipid catabolic processCytosolic phospholipase A2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
lysophospholipase activityCytosolic phospholipase A2Homo sapiens (human)
phospholipase A2 activityCytosolic phospholipase A2Homo sapiens (human)
calcium ion bindingCytosolic phospholipase A2Homo sapiens (human)
calcium-dependent phospholipid bindingCytosolic phospholipase A2Homo sapiens (human)
O-acyltransferase activityCytosolic phospholipase A2Homo sapiens (human)
phosphatidylinositol-5-phosphate bindingCytosolic phospholipase A2Homo sapiens (human)
phosphatidylinositol-3-phosphate bindingCytosolic phospholipase A2Homo sapiens (human)
calcium-dependent phospholipase A2 activityCytosolic phospholipase A2Homo sapiens (human)
calcium-independent phospholipase A2 activityCytosolic phospholipase A2Homo sapiens (human)
phosphatidylinositol-4-phosphate bindingCytosolic phospholipase A2Homo sapiens (human)
phosphatidyl phospholipase B activityCytosolic phospholipase A2Homo sapiens (human)
ceramide 1-phosphate bindingCytosolic phospholipase A2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
Golgi membraneCytosolic phospholipase A2Homo sapiens (human)
nuclear envelopeCytosolic phospholipase A2Homo sapiens (human)
cytoplasmCytosolic phospholipase A2Homo sapiens (human)
mitochondrial inner membraneCytosolic phospholipase A2Homo sapiens (human)
endoplasmic reticulum membraneCytosolic phospholipase A2Homo sapiens (human)
cytosolCytosolic phospholipase A2Homo sapiens (human)
intracellular membrane-bounded organelleCytosolic phospholipase A2Homo sapiens (human)
nucleusCytosolic phospholipase A2Homo sapiens (human)
endoplasmic reticulumCytosolic phospholipase A2Homo sapiens (human)
Golgi apparatusCytosolic phospholipase A2Homo sapiens (human)
cytosolCytosolic phospholipase A2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (57)

Assay IDTitleYearJournalArticle
AID404477Inhibition of TXB2 production in Sprague-Dawley rat whole blood2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404499Plasma concentration in adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po after 16 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID315906Inhibition of cPLA2-alpha in Sprague-Dawley rat whole blood assay in presence of A231872008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
AID404479Inhibition of LTB4 production in mouse MC9 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404510Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID345899Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 15 mg/kg, iv2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID345901Inhibition of human cytosolic PLA2alpha by GLU micelle assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID404502Inhibition of acute hyperresponsiveness in Ascaris Suum antigen-induced reversible airway bronchoconstriction sheep model assessed as reduction in lung resistance at 10 mg/kg, po bid administered 8 hrs before antigen challenge and measured after 16 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404481Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404493Plasma concentration in collagen-induced arthritis mouse model at 100 mg/kg, po twice daily after 3 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404497Plasma concentration in adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po after 16 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404506Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404461Inhibition of secreted phospholipase A2 at 0.5 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404498Plasma concentration in adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po after 16 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID315908Oral bioavailability in Sprague-Dawley rat at 25 mg/kg administered through MC/TW formulation2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
AID1187022Antiinflammatory activity in C57BL/6 mouse assessed as reduction of TPA-induced ear thickness at 50 mg/kg, po treated 30 mins prior to TPA challenge2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
AID1187020Antiinflammatory activity against C3H/HeN mouse abdominal cavity cells assessed as inhibition of LPS-induced PGE2 production after 6 hrs by EIA2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
AID404456Plasma concentration in adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po after 4 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404490Inhibition of PGF2alpha production in human whole blood at 0.15 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404507Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404459Inhibition of cytosolic phospholipase A2gamma at 0.5 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404476Inhibition of cytosolic phospholipase A2alpha by GLU micelle assay2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404487Inhibition of TXB2 production in human whole blood at 0.15 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404489Inhibition of PGE2 production in human whole blood at 0.15 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID345902Inhibition of A23187-induced TBX2 release in Sprague-Dawley rat whole blood2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID404460Inhibition of cytosolic phospholipase A2alpha2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404458Inhibition of cytosolic phospholipase A2beta at 0.5 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1187018Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
AID404505Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID315909Oral bioavailability in Sprague-Dawley rat at 25 mg/kg administered through Phosal formulation2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
AID404495Plasma concentration in adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po after 4 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404480Inhibition of PGF2alpha production in mouse MC9 cells2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404504Ratio of AUC in Sprague-Dawley rat at 25 mg/kg, po to IC50 for TXB2 production in Sprague-Dawley rat whole blood2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404468Inhibition of COX1 in microsomes at 100 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID430184Inhibition of cytosolic phospholipase A2alpha by GLU micelle assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties.
AID404496Plasma concentration in adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po after 4 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404472Inhibition of PGE2 production in carrageenan-stimulated orally dosed rat air pouch model after 6 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404509Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404491Inhibition of PAF production in human whole blood at 0.15 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID315907Clearance in Sprague-Dawley rat at 2 mg/kg, iv2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
AID1187028Inhibition of A23187-induced TXB2 generation in human whole blood by EIA2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
AID404457Inhibition of cytosolic phospholipase A2alpha at 0.020 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404469Oral bioavailability in rat2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID315905Inhibition of human cPLA2-alpha assessed as cleavage of 7-hydroxycoumarinyl-gamma-linolenate2008Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
AID404478Plasma clearance in Sprague-Dawley rat at 2 mg/kg, iv2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1187027Inhibition of A23187-induced TXB2 generation in Hartley guinea pig whole blood by EIA2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
AID404503Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells at 0.040 uM in presence of arachidonic acid2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404494Plasma concentration in collagen-induced arthritis mouse model at 100 mg/kg, po twice daily after 12 to 14 hrs2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404500Effect on early asthmatic response in Ascaris Suum antigen-induced reversible airway bronchoconstriction sheep model at 10 mg/kg, po bid administered 24 hrs before antigen challenge2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404475Inhibition of carrageenan-induced paw edema in po dosed Sprague-Dawley rat administered 2 hrs before carrageenan challenge2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404508Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po for 11 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404467Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells at 0.040 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404465Inhibition of COX2 in microsomes at 100 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID346090Plasma concentration in carrageenan-induced paw edema Sprague-Dawley rat model at 10 mg/kg, iv2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
AID404501Effect on late asthmatic response in Ascaris Suum antigen-induced reversible airway bronchoconstriction sheep model assessed as reduction in lung resistance at 10 mg/kg, po bid administered 2 hrs before antigen challenge measured 5 to 8 hrs after challeng2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID404488Inhibition of LTB4 production in human whole blood at 0.15 uM2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
AID1187019Partition coefficient, log P of the compound by reversed phase HPLC analysis2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (62.50)29.6817
2010's3 (37.50)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: 12.20

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 Index12.20 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.20)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]