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hesperetin (CID 72281) - Compound BioActivity Data
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BioActivity Outcomes:
Active(29)
 
 
Inactive(635)
 
 
Inconclusive(61)
 
 
Unspecified(75)
 
 
Top Targets:
7TM GPCR Srx(22)
 
 
 
p450(17)
 
 
 
 
7TM GPCR Srsx(15)
 
 
HSD10-like SD..(8)
 
 
 
NR LBD PPAR(8)
 
 
 
BioAssay Types:
Screening(332)
 
 
 
Confirmatory(295)
 
 
 
 
 
Literature(98)
 
 
 
 
 
BioActivity Types:
Potency(235)
 
 
 
 
 
IC50(23)
 
 
 
 
 
EC50(7)
 
 
Ki(2)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 654    Data Row: 800   Total Pages: 16   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103558713]
IC50 0.511Inhibition of human CYP1B1 by EROD assay [AID502475, Type: Literature]Cytochrome P450 1B1 [gi:48429256]
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2
[SID103558713]
IC50 2.1Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs [AID400608, Type: Literature]
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3
[SID103558713]
IC50 2.786Inhibition of human CYP1A1 by EROD assay [AID502474, Type: Literature]Cytochrome P450 1A1 [gi:117139]
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4
[SID11112384]
Potency 5.0119qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
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5
[SID11112384]
Potency 5.0119qHTS Assay for Identification of Small Molecule Antagonists for Hypoxia Response Element Signaling Pathway [AID915, Type: confirmatory]hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) [Homo sapiens] [gi:32879895]
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6
[SID11112385]
Potency 7.9433qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C19 [AID899, Type: confirmatory]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
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7
[SID11112384]
Potency 10qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2C9 [AID883, Type: confirmatory]cytochrome P450 2C9 precursor [Homo sapiens] [gi:13699818]
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8
[SID56463566]
Potency 15.1014qHTS profiling assay for firefly luciferase inhibitor/activator using purifed enzyme and Km concentrations of substrates (counterscreen for miR-21 project) [AID588342, Type: confirmatory]Luciferase [Photinus pyralis] [gi:160794]
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9
[SID26754195]
Potency 15.8489qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4 [AID884, Type: confirmatory]cytochrome P450 3A4 isoform 1 [Homo sapiens] [gi:13435386]
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10
[SID103558713]
ID50 20.9Inhibition of Moloney murine leukemia virus reverse transcriptase using (riboadenylic acid)n(deoxythymidylic acid)12-18 as template primer by liquid scintillation counting [AID339056, Type: Literature]
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11
[SID103558713]
ID50 22.1Inhibition of Moloney murine leukemia virus reverse transcriptase using (ribocytidylic acid)n(deoxyguanylic acid)12-18 as template primer by liquid scintillation counting [AID339057, Type: Literature]
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12
[SID103558713]
IC50 34.647Inhibition of human CYP1A2 by EROD assay [AID502473, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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13
[SID11112384]
Cytochrome panel assay with activity outcomes [AID1851_1, Type: other]cytochrome P450 2C19 precursor [Homo sapiens] [gi:4503219]
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14
[SID11112384]
Cytochrome panel assay with activity outcomes [AID1851_5, Type: other]cytochrome P450 2C9 precursor [Homo sapiens] [gi:13699818]
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15
[SID103558713]
Induction of PPARgamma-mediated ABCA1 promoter activity in human THP1 cells after 24 hrs by luciferase reporter gene analysis [AID663328, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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16
[SID103558713]
Induction of LXRalpha-mediated ABCA1 promoter activity in human THP1 cells after 24 hrs by luciferase reporter gene analysis [AID663324, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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17
[SID103558713]
Increase in LXRalpha-mediated ABCA1 mRNA expression in human THP1 cells at 5 to 15 uM after 24 hrs by RT-PCR analysis [AID663325, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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18
[SID103558713]
Increase in LXRalpha-mediated ABCA1 protein expression in human THP1 cells at 5 to 15 uM after 48 hrs by Western blotting analysis [AID663326, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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19
[SID56463566]
Screen for inhibitors of the SWI/SNF chromatin remodeling complex (esBAF) in mouse embryonic stem cells with Luciferase reporter assay Measured in Cell-Based System Using Plate Reader - 2141-01_Inhibitor_SinglePoint_HTS_Activity [AID602393, Type: screening]transcription activator BRG1 isoform 1 [Mus musculus] [gi:291463269]
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20
[SID103558713]
Antagonist activity at human TGF-beta receptor in HeLa cells assessed as reduction in TGF-beta1-induced Smad3 phosphorylation at 100 uM after 1 hr by Western blot analysis [AID717764, Type: Literature]
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21
[SID103558713]
Antagonist activity at human TGF-beta receptor in HeLa cells assessed as suppression of nuclear translocation of Smad3 at 100 uM after 1 hr by immunofluorescence imaging [AID717765, Type: Literature]
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22
[SID103558713]
Antagonist activity at human TGF-beta receptor in HeLa cells assessed as reduction in TGF-beta1-induced p21 expression at 100 uM after 24 hrs by Western blot analysis [AID717766, Type: Literature]
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23
[SID103558713]
Antimigratory activity against human HeLa cells assessed as inhibition of TGF-beta1-induced cell migration at 100 uM after 24 hrs by scratch motility assay [AID717767, Type: Literature]
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24
[SID103558713]
Antimigratory activity against human HeLa cells assessed as inhibition of TGF-beta1-induced cell invasion across collagen matrix at 100 uM after 1 hr by collagen-based cell Invasion assay [AID717768, Type: Literature]
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25
[SID56463566]
Wnt/Beta-catenin HTS Measured in Cell-Based System Using Plate Reader - 2161-01_Activator_SinglePoint_HTS_Activity [AID743398, Type: screening]
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26
[SID11112384]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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27
[SID11112384]
Cytochrome panel assay with activity outcomes [AID1851_4, Type: other]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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28
[SID11112385]
p450-cyp1a2 [AID410, Type: confirmatory]cytochrome P450 1A2 [Homo sapiens] [gi:73915100]
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29
[SID103558713]
Displacement of biotinylated TGF-beta1 from human TGF-beta type 2 receptor at 100 uM after 1 hr by avidin-FITC-based flow cytometry [AID717762, Type: Literature]TGF-beta receptor type-2 [gi:116242818]
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30
[SID103558713]
EC50 10Cytotoxicity against human RPMI8226 cells assessed as viable cells after 72 hrs by calcein AM assay [AID477847, Type: Literature]
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31
[SID103558713]
EC50 10Cytotoxicity against human U266 cells assessed as viable cells after 72 hrs by calcein AM assay [AID477848, Type: Literature]
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32
[SID103558713]
EC50 10Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay [AID477849, Type: Literature]
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33
[SID103558713]
EC50 10Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay [AID477850, Type: Literature]
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34
[SID103558713]
EC50 10Cytotoxicity against human THP1 cells after 72 hrs by erythosin B staining method [AID477851, Type: Literature]
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35
[SID103558713]
EC50 10Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay [AID477845, Type: Literature]
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36
[SID103558713]
EC50 10Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay [AID477846, Type: Literature]
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37
[SID103558713]
IC50 1774.1Inhibition of equine BChE assessed as butyrylthiocholine iodide hydrolysis after 10 mins preincubation by spectrophotometry [AID654701, Type: Literature]Butyrylcholinesterase [gi:75074633]
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38
[SID103558713]
IC50 2476.1Inhibition of human erythrocyte AChE assessed as acetylthiocholine iodide hydrolysis after 10 mins preincubation by spectrophotometry [AID654699, Type: Literature]Acetylcholinesterase [gi:113037]
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39
[SID56463566]
Potency qHTS for Inhibitors of Human Acid Sphingomyelinase Assay: Native Substrate [AID624178, Type: confirmatory]acid sphingomyelinase [Homo sapiens] [gi:179095]
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40
[SID103558713]
Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as beta-galactosidase activity at 50 uM measured after 48 hrs relative to vehicle control [AID736341, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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41
[SID103558713]
Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as beta-galactosidase activity at 25 uM measured after 48 hrs relative to vehicle control [AID736345, Type: Literature]Peroxisome proliferator-activated receptor delta [gi:417522]
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42
[SID103558713]
Induction of ApoA1-mediated cholestrol efflux in human THP1 cells after 12 hrs by fluorometric analysis [AID663329, Type: Literature]Apolipoprotein A-I [gi:113992]
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43
[SID103558713]
Agonist activity at human PPARgamma expressed in HEK293 cells co-transfected with PPRE assessed as beta-galactosidase signal at 5 uM after 48 hrs by reporter gene assay relative to control [AID439367, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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44
[SID103558713]
Agonist activity at human PPARgamma expressed in HEK293 cells co-transfected with PPRE assessed as beta-galactosidase signal at 25 uM after 48 hrs by reporter gene assay relative to control [AID439368, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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45
[SID103558713]
Induction of PPARgamma enhancer activity in human THP1 cells after 24 hrs by luciferase reporter gene analysis [AID663327, Type: Literature]Peroxisome proliferator-activated receptor gamma [gi:13432234]
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46
[SID103558713]
Inhibition of human recombinant 17beta-HSD2 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol at 40 uM [AID406996, Type: Literature]Estradiol 17-beta-dehydrogenase 2 [gi:544152]
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47
[SID103558713]
Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay [AID311281, Type: Literature]Mu-type opioid receptor [gi:2851402]
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48
[SID103558713]
Agonist activity at human PPARalpha expressed in HEK293 cells co-transfected with PPRE assessed as beta-galactosidase signal at 25 uM after 48 hrs by reporter gene assay relative to control [AID439371, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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49
[SID103558713]
Agonist activity at human PPARalpha expressed in HEK293 cells co-transfected with PPRE assessed as beta-galactosidase signal at 40 uM after 48 hrs by reporter gene assay relative to control [AID439372, Type: Literature]Peroxisome proliferator-activated receptor alpha [gi:3041727]
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50
[SID103558713]
Inhibition of mushroom tyrosinase at 100 uM preincubated for 10 mins before addition of 1.7 mM L-tyrosine measured after 20 mins by spectrophotometric method [AID587206, Type: Literature]Polyphenol oxidase 2 [gi:6686057]
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