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sulindac sulfide (CID 5352624) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(30)
 
 
Inactive(113)
 
 
Inconclusive(40)
 
 
Unspecified(183)
 
 
Top Targets:
7TM GPCR Srsx(17)
 
 
 
 
7TM GPCR Srx(17)
 
 
 
NR LBD PPAR(12)
 
 
 
 
 
p450(10)
 
 
 
 
prostaglandin..(10)
 
 
 
 
BioAssay Types:
Confirmatory(119)
 
 
 
 
Literature(82)
 
 
 
 
Summary(24)
 
 
 
 
Screening(9)
 
 
BioActivity Types:
IC50(138)
 
 
 
 
Potency(126)
 
 
 
 
EC50(10)
 
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 356    Data Row: 366   Total Pages: 8   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103183701]
IC50 0.05Inhibition of ovine COX1 after 5 mins [AID492859, Type: Literature]Prostaglandin G/H synthase 1 [gi:548481]
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2
[SID103183701]
IC50 0.084DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) [AID625208, Type: other]Aldose reductase [gi:1168407]
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3
[SID103183701]
IC50 0.1Inhibition of human recombinant COX2 after 5 mins [AID492858, Type: Literature]Prostaglandin G/H synthase 2 [gi:3915797]
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4
[SID103183701]
IC50 0.115Inhibition of COX1 [AID675695, Type: Literature]
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5
[SID103183701]
IC50 0.14Inhibition of COX2 [AID675696, Type: Literature]
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6
[SID103183701]
IC50 0.688DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) [AID625243, Type: other]Prostaglandin G/H synthase 1 [gi:317373262]
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7
[SID103183701]
EC50 0.8Agonist activity at PPARgamma expressed in human HCA7 cells assessed as induction of peroxisome proliferator response element after 12 hrs by luciferase reporter assay [AID361858, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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8
[SID103183701]
IC50 1.092DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) [AID625181, Type: other]Mitogen-activated protein kinase 1 [gi:119554]
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9
[SID103183701]
IC50 1.537DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) [AID625244, Type: other]Prostaglandin G/H synthase 2 [gi:3915797]
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10
[SID103183701]
IC50 2DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625245, Type: other]Cytochrome P450 1A2 [gi:117144]
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11
[SID144207185]
Ratio Potency (uM) 2.485qHTS assay to identify small molecule agonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathway: Summary [AID743140, Type: summary]peroxisome proliferator activated receptor gamma [Homo sapiens] [gi:216409692]
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12
[SID103183701]
Ki 3.5Binding affinity towards human CRTH2 receptor expressed in CHO cells [AID254359, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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13
[SID103183701]
IC50 7.231DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) [AID625196, Type: other]Adenosine receptor A3 [gi:1351831]
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14
[SID144207185]
Potency-Replicate_1 9.4392qHTS assay to identify small molecule that activate the aryl hydrocarbon receptor (AhR) signaling pathway [AID743085, Type: confirmatory]aryl hydrocarbon receptor [Homo sapiens] [gi:51095037]
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15
[SID144207185]
AhR Potency (uM) 16.1535qHTS assay to identify small molecule that activate the aryl hydrocarbon receptor (AhR) signaling pathway: Summary [AID743122, Type: summary]aryl hydrocarbon receptor [Homo sapiens] [gi:51095037]
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16
[SID103183701]
IC50 23.981DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) [AID625184, Type: other]Epidermal growth factor receptor [gi:2811086]
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17
[SID144207185]
Potency-Replicate_1 26.6032qHTS assay for small molecule agonists of the p53 signaling pathway - cell viability [AID651633, Type: confirmatory]
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18
[SID144207185]
TR Potency (uM) 26.6032qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway: Summary [AID743067, Type: summary]thyroid hormone receptor beta isoform 2 [Rattus norvegicus] [gi:399498506]
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19
[SID103183701]
IC50 27.822DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) [AID625252, Type: other]D(1A) dopamine receptor [gi:118228]
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20
[SID103183701]
IC50 29.368DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) [AID625145, Type: other]Cysteinyl leukotriene receptor 1 [gi:20138087]
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21
[SID103183701]
IC50 33.668DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) [AID625163, Type: other]Mu-type opioid receptor [gi:2851402]
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22
[SID103183701]
IC50 34Inhibition of gamma secretase assessed as reduction in Abeta42 production [AID692103, Type: Literature]
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23
[SID103183701]
IC50 34Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA [AID492867, Type: Literature]
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24
[SID103183701]
IC50 38.7Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay [AID535977, Type: Literature]
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25
[SID26755246]
Potency 44.6684Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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26
[SID103183701]
IC50 45.2Displacement of [3H]L685458 from human SPP expressed in HEK293 cells [AID329705, Type: Literature]
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27
[SID103183701]
Drug level in mouse brain at 50 mg/kg, po [AID263727, Type: Literature]
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28
[SID103183701]
Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation at 0.1 uM after 96 hrs by haemocytometry [AID535985, Type: Literature]
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29
[SID103183701]
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation at 0.1 uM after 96 hrs by haemocytometry [AID536074, Type: Literature]
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30
[SID170466724]
qHTS assay to identify small molecule antagonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathway: Summary [AID743199, Type: summary]peroxisome proliferator activated receptor gamma [Homo sapiens] [gi:216409692]
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31
[SID103183701]
IC50 53Inhibition of gamma-secretase in HEK293 cells co-overexpressing NotchdeltaE assessed as inhibition of notch cleavage by luciferase reporter gene assay [AID501318, Type: Literature]
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32
[SID103183701]
IC50 57.1Displacement of [3H]L685458 from gamma-secretase in human THP1 cells [AID329706, Type: Literature]
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33
[SID103183701]
IC50 80Inhibition of mPGES1 [AID405533, Type: Literature]
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34
[SID103183701]
IC50 82.5Inhibition of gamma-secretase in HEK293 cells co-overexpressing APP Swedish mutant assessed as inhibition of amyloid beta 42 production by luciferase reporter gene assay [AID501317, Type: Literature]
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35
[SID103183701]
IC50 146Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay [AID535976, Type: Literature]
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36
[SID103183701]
IC50 180Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells [AID105636, Type: Literature]
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37
[SID103183701]
IC50 200Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line [AID105980, Type: Literature]
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38
[SID103183701]
IC50 200Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF) [AID166562, Type: Literature]
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39
[SID103183701]
IC50 200Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells [AID202033, Type: Literature]
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40
[SID103183701]
EC50 209Cytotoxicity against human MDA-MB-231 cells after 48 hrs by WST1 assay [AID675702, Type: Literature]
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41
[SID103183701]
IC50 215Inhibition of gamma-secretase in HEK293 cells co-overexpressing APP Swedish mutant assessed as inhibition of amyloid beta 40 production by luciferase reporter gene assay [AID501316, Type: Literature]
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42
[SID103183701]
IC50 332Displacement of [3H]IN973 from gamma-secretase in human THP1 cells [AID329707, Type: Literature]
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43
[SID103183701]
IC50 350Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts [AID144345, Type: Literature]
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44
[SID103183701]
Drug level in mouse plasma at 50 mg/kg, po [AID263728, Type: Literature]
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45
[SID103183701]
Ratio of drug level in brain against plasma in mice at 50 mg/kg, po [AID263729, Type: Literature]
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46
[SID103183701]
Inhibition of p21ras protein and Raf kinase in vitro using recombinant proteins [AID223804, Type: Literature]
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47
[SID103183701]
Inhibition of beta amyloid protein 42 in HEK cell lines overexpressing APP695 at 40 uM [AID263721, Type: Literature]
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48
[SID103183701]
Half-maximal inhibition of the COX activity was measured by the direct analysis of the consumed O2 using isolated sheep seminal vesicles [AID54368, Type: Literature]
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49
[SID103183701]
The compound was evaluated for percent incorporation in DOPC vesicles, when compound to lipid mol ratio is 0.1 [AID104152, Type: Literature]
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50
[SID103183701]
The compound was evaluated for percent incorporation in DOPC vesicles, when compound to lipid mol ratio is 2 [AID104153, Type: Literature]
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