Assay ID | Title | Year | Journal | Article |
AID404477 | Inhibition of TXB2 production in Sprague-Dawley rat whole blood | 2008 | Journal 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. |
AID404499 | Plasma concentration in adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po after 16 hrs | 2008 | Journal 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. |
AID315906 | Inhibition of cPLA2-alpha in Sprague-Dawley rat whole blood assay in presence of A23187 | 2008 | Bioorganic & 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. |
AID404479 | Inhibition of LTB4 production in mouse MC9 cells | 2008 | Journal 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. |
AID404510 | Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po for 11 days | 2008 | Journal 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. |
AID345899 | Antiinflammatory activity against carrageenan-induced paw edema in Sprague-Dawley rat at 15 mg/kg, iv | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. |
AID345901 | Inhibition of human cytosolic PLA2alpha by GLU micelle assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. |
AID404502 | Inhibition 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 hrs | 2008 | Journal 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. |
AID404481 | Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells | 2008 | Journal 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. |
AID404493 | Plasma concentration in collagen-induced arthritis mouse model at 100 mg/kg, po twice daily after 3 hrs | 2008 | Journal 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. |
AID404497 | Plasma concentration in adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po after 16 hrs | 2008 | Journal 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. |
AID404506 | Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po for 11 days | 2008 | Journal 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. |
AID404461 | Inhibition of secreted phospholipase A2 at 0.5 uM | 2008 | Journal 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. |
AID404498 | Plasma concentration in adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po after 16 hrs | 2008 | Journal 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. |
AID315908 | Oral bioavailability in Sprague-Dawley rat at 25 mg/kg administered through MC/TW formulation | 2008 | Bioorganic & 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. |
AID1187022 | Antiinflammatory activity in C57BL/6 mouse assessed as reduction of TPA-induced ear thickness at 50 mg/kg, po treated 30 mins prior to TPA challenge | 2014 | Journal 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. |
AID1187020 | Antiinflammatory activity against C3H/HeN mouse abdominal cavity cells assessed as inhibition of LPS-induced PGE2 production after 6 hrs by EIA | 2014 | Journal 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. |
AID404456 | Plasma concentration in adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po after 4 hrs | 2008 | Journal 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. |
AID404490 | Inhibition of PGF2alpha production in human whole blood at 0.15 uM | 2008 | Journal 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. |
AID404507 | Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po for 11 days | 2008 | Journal 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. |
AID404459 | Inhibition of cytosolic phospholipase A2gamma at 0.5 uM | 2008 | Journal 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. |
AID404476 | Inhibition of cytosolic phospholipase A2alpha by GLU micelle assay | 2008 | Journal 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. |
AID404487 | Inhibition of TXB2 production in human whole blood at 0.15 uM | 2008 | Journal 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. |
AID404489 | Inhibition of PGE2 production in human whole blood at 0.15 uM | 2008 | Journal 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. |
AID345902 | Inhibition of A23187-induced TBX2 release in Sprague-Dawley rat whole blood | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. |
AID404460 | Inhibition of cytosolic phospholipase A2alpha | 2008 | Journal 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. |
AID404458 | Inhibition of cytosolic phospholipase A2beta at 0.5 uM | 2008 | Journal 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. |
AID1187018 | Inhibition 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 counting | 2014 | Journal 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. |
AID404505 | Reduction in synovitis damage in Freund's adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po for 11 days | 2008 | Journal 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. |
AID315909 | Oral bioavailability in Sprague-Dawley rat at 25 mg/kg administered through Phosal formulation | 2008 | Bioorganic & 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. |
AID404495 | Plasma concentration in adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po after 4 hrs | 2008 | Journal 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. |
AID404480 | Inhibition of PGF2alpha production in mouse MC9 cells | 2008 | Journal 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. |
AID404504 | Ratio of AUC in Sprague-Dawley rat at 25 mg/kg, po to IC50 for TXB2 production in Sprague-Dawley rat whole blood | 2008 | Journal 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. |
AID404468 | Inhibition of COX1 in microsomes at 100 uM | 2008 | Journal 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. |
AID430184 | Inhibition of cytosolic phospholipase A2alpha by GLU micelle assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
| Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties. |
AID404496 | Plasma concentration in adjuvant-induced arthritis Lewis rat model at 5 mg/kg, po after 4 hrs | 2008 | Journal 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. |
AID404472 | Inhibition of PGE2 production in carrageenan-stimulated orally dosed rat air pouch model after 6 hrs | 2008 | Journal 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. |
AID404509 | Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 25 mg/kg, po for 11 days | 2008 | Journal 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. |
AID404491 | Inhibition of PAF production in human whole blood at 0.15 uM | 2008 | Journal 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. |
AID315907 | Clearance in Sprague-Dawley rat at 2 mg/kg, iv | 2008 | Bioorganic & 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. |
AID1187028 | Inhibition of A23187-induced TXB2 generation in human whole blood by EIA | 2014 | Journal 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. |
AID404457 | Inhibition of cytosolic phospholipase A2alpha at 0.020 uM | 2008 | Journal 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. |
AID404469 | Oral bioavailability in rat | 2008 | Journal 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. |
AID315905 | Inhibition of human cPLA2-alpha assessed as cleavage of 7-hydroxycoumarinyl-gamma-linolenate | 2008 | Bioorganic & 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. |
AID404478 | Plasma clearance in Sprague-Dawley rat at 2 mg/kg, iv | 2008 | Journal 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. |
AID1187027 | Inhibition of A23187-induced TXB2 generation in Hartley guinea pig whole blood by EIA | 2014 | Journal 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. |
AID404503 | Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells at 0.040 uM in presence of arachidonic acid | 2008 | Journal 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. |
AID404494 | Plasma concentration in collagen-induced arthritis mouse model at 100 mg/kg, po twice daily after 12 to 14 hrs | 2008 | Journal 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. |
AID404500 | Effect 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 challenge | 2008 | Journal 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. |
AID404475 | Inhibition of carrageenan-induced paw edema in po dosed Sprague-Dawley rat administered 2 hrs before carrageenan challenge | 2008 | Journal 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. |
AID404508 | Reduction in cartilage damage in Freund's adjuvant-induced arthritis Lewis rat model at 50 mg/kg, po for 11 days | 2008 | Journal 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. |
AID404467 | Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells at 0.040 uM | 2008 | Journal 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. |
AID404465 | Inhibition of COX2 in microsomes at 100 uM | 2008 | Journal 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. |
AID346090 | Plasma concentration in carrageenan-induced paw edema Sprague-Dawley rat model at 10 mg/kg, iv | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. |
AID404501 | Effect 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 challeng | 2008 | Journal 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. |
AID404488 | Inhibition of LTB4 production in human whole blood at 0.15 uM | 2008 | Journal 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. |
AID1187019 | Partition coefficient, log P of the compound by reversed phase HPLC analysis | 2014 | Journal 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] |