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TO-901317 (CID 447912) - Compound BioActivity Data
.
BioActivity Outcomes:
Probe(2)
 
 
Active(165)
 
 
Inactive(341)
 
 
Inconclusive(39)
 
 
Unspecified(104)
 
 
Top Targets:
NR LBD LXR(112)
 
 
 
 
 
NR LBD PPAR(15)
 
 
 
7TM GPCR Srsx(10)
 
 
NR LBD ROR li..(9)
 
 
 
 
NR LBD TR(8)
 
 
 
BioAssay Types:
Literature(264)
 
 
 
 
 
Screening(244)
 
 
 
 
Confirmatory(129)
 
 
 
 
 
Summary(2)
 
 
BioActivity Types:
Potency(124)
 
 
 
 
 
EC50(77)
 
 
 
IC50(39)
 
 
 
 
AC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 539    Data Row: 651   Total Pages: 14   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID85257301]
Summary of probe development efforts to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR). [AID2139, Type: summary]nuclear receptor ROR-alpha isoform a [Homo sapiens] [gi:19743903]
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2
[SID85257301]
Summary of probe development efforts to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR). [AID2139, Type: summary]nuclear receptor ROR-gamma isoform a [Homo sapiens] [gi:19743909]
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3
[SID103249306]
EC50 0.003Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL [AID452973, Type: Literature]
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4
[SID103249306]
EC50 0.003Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO901317 [AID452974, Type: Literature]
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5
[SID103249306]
EC50 0.003Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL [AID345492, Type: Literature]
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6
[SID103249306]
EC50 0.0032Agonist activity at LXRalpha by TR-FRET assay [AID569814, Type: Literature]
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7
[SID103249306]
EC50 0.0047Agonist activity at LXRbeta by TR-FRET assay [AID569815, Type: Literature]
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8
[SID103249306]
EC50 0.008Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay [AID418425, Type: Literature]
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9
[SID103249306]
IC50 0.009Displacement of [3H]T0901317 from LXRbeta ligand binding domain [AID478580, Type: Literature]
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10
[SID103249306]
IC50 0.009Displacement of [3H]T0901317 from human recombinant LXRalpha-LBD [AID451978, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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11
[SID103249306]
IC50 0.009Displacement of [3H]T0901317 from human recombinant LXRalpha LBD [AID454631, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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12
[SID103249306]
IC50 0.009Displacement of [3H]T0901317 from human recombinant LXRalpha LBD [AID454924, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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13
[SID103249306]
IC50 0.009Displacement of [3H]T0901317 from human recombinant LXRbeta ligand binding domain [AID452860, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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14
[SID103249306]
IC50 0.009Binding affinity to human recombinant LXRbeta ligand binding domain [AID472479, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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15
[SID103249306]
IC50 0.009Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method [AID452959, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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16
[SID103249306]
IC50 0.009Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method [AID345471, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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17
[SID103249306]
IC50 0.009Binding affinity at human LXRbeta [AID313446, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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18
[SID103249306]
IC50 0.01Displacement of [3H]T-0901317 from human LXR beta receptor [AID273407, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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19
[SID103249306]
IC50 0.01Displacement of [3H]T-0901317 from human LXR alpha receptor [AID273406, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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20
[SID103249306]
EC50 0.01Activity against LXR alpha transiently transfected in HEK293 cells [AID262339, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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21
[SID103249306]
EC50 0.01Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay [AID418426, Type: Literature]
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22
[SID103249306]
EC50 0.011Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay [AID307304, Type: Literature]
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23
[SID103249306]
EC50 0.011Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay [AID299789, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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24
[SID103249306]
IC50 0.013Displacement of [3H]T0901317 from human recombinant LXRbeta-LBD [AID451979, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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25
[SID103249306]
IC50 0.013Displacement of [3H]T0901317 from human recombinant LXRbeta LBD [AID454925, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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26
[SID103249306]
IC50 0.013Displacement of [3H]T0901317 from human recombinant LXRbeta LBD [AID454632, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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27
[SID103249306]
IC50 0.013Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method [AID345472, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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28
[SID103249306]
IC50 0.013Binding affinity to human recombinant LXRalpha ligand binding domain [AID472480, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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29
[SID103249306]
IC50 0.013Binding affinity at human LXRalpha [AID313447, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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30
[SID103249306]
IC50 0.013Displacement of [3H]T0901317 from human recombinant LXRalpha ligand binding domain [AID452861, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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31
[SID103249306]
IC50 0.013Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method [AID452960, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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32
[SID103249306]
IC50 0.013Displacement of [3H]T0901317 from LXRalpha ligand binding domain [AID478581, Type: Literature]
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33
[SID103249306]
EC50 0.015Agonist activity at LXRbeta LBD by HTRF cofactor peptide recruitment assay [AID307303, Type: Literature]
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34
[SID103249306]
EC50 0.015Agonist activity at human LXRbeta receptor after 1 hr by HTRF cofactor recruitment assay [AID299787, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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35
[SID103249306]
EC50 0.016Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay [AID273408, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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36
[SID103249306]
EC50 0.016Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay [AID452863, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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37
[SID103249306]
EC50 0.019Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation [AID472470, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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38
[SID103249306]
IC50 0.01995Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay [AID474683, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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39
[SID103249306]
EC50 0.027Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression [AID452866, Type: Literature]
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40
[SID103249306]
EC50 0.03Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor) [AID240219, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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41
[SID103249306]
IC50 0.03Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domain [AID391700, Type: Literature]Oxysterols receptor LXR-beta [gi:296439251]
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42
[SID103249306]
IC50 0.03Binding affinity to LXRalpha by radioligand displacement assay [AID271504, Type: Literature]Oxysterols receptor LXR-alpha [gi:23503089]
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43
[SID103249306]
EC50 0.033Induction of cholesterol efflux in THP1 cells after 18 hrs [AID307307, Type: Literature]
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44
[SID103249306]
EC50 0.033Induction of cholesterol efflux in THP1 cells [AID299793, Type: Literature]
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45
[SID103249306]
EC50 0.034Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR [AID424924, Type: Literature]
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46
[SID103249306]
EC50 0.035Effect on ABCA1 gene expression in mouse J774 cells [AID313456, Type: Literature]
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47
[SID103249306]
EC50 0.035Induction of ABCA1 mRNA expression in mouse J774A1 cells [AID451983, Type: Literature]
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48
[SID103249306]
EC50 0.035Induction of ABCA1 mRNA upregulation in human THP1 cells [AID454927, Type: Literature]
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49
[SID103249306]
EC50 0.035Upregulation of ABCA1 mRNA level in mouse J774 cells [AID478586, Type: Literature]
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50
[SID103249306]
EC50 0.036Upregulation of SREB1c mRNA level in human HuH7 cells [AID478588, Type: Literature]
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