Sirolimus (CID 5284616) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(365)
 
 
Inactive(99)
 
 
Inconclusive(10)
 
 
Unspecified(827)
 
 
Top Targets:
PKc like(18)
 
 
7TM GPCR Srx(12)
 
 
PKc(10)
 
 
PIKKc TOR(10)
 
 
 
 
7TM GPCR Srsx(10)
 
 
BioAssay Types:
Literature(637)
 
 
 
 
 
Confirmatory(47)
 
 
 
 
 
Screening(5)
 
 
BioActivity Types:
IC50(490)
 
 
 
Potency(46)
 
 
 
 
 
EC50(6)
 
 
Ki(3)
 
 
Kd(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1123    Data Row: 1301   Total Pages: 27   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103164548]
EC50 0.0001Antiviral activity against HIV1 R5 assessed as inhibition of cell-cell fusion between R5-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days [AID406211, Type: Literature]
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2
[SID103164548]
IC50 0.0001Inhibition of mTOR kinase expressed in human HEK293 cells by western blot analysis [AID360764, Type: Literature]Serine/threonine-protein kinase mTOR [gi:1169735]
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3
[SID103164548]
IC50 0.0001Inhibition of mTOR kinase expressed in human HEK293 cells by western blot analysis [AID360764, Type: Literature]Serine/threonine-protein kinase mTOR [gi:1169735]
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4
[SID103164548]
EC50 0.00015Antiviral activity against HIV1 ADA in human PBMC assessed as reduction of p24 antigen levels [AID406215, Type: Literature]
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5
[SID103164548]
EC50 0.00018Antiviral activity against HIV1 R5 in human PBMC assessed as fractional inhibition of viral replication [AID406228, Type: Literature]
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6
[SID103164548]
Ki 0.0002Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity [AID69108, Type: Literature]
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7
[SID103164548]
IC50 0.00045Inhibitory concentration against binding to FKBP12 [AID254768, Type: Literature]
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8
[SID103164548]
IC50 0.00045Inhibitory concentration against FKBP12 receptor [AID254831, Type: Literature]
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9
[SID103164548]
IC50 0.0005Immunosuppressive activity was evaluated by the inhibition of human T-lymphocyte proliferation [AID209953, Type: Literature]
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10
[SID103164548]
Ki 0.0005Binding affinity for FK506 binding protein [AID69098, Type: other]
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11
[SID103164548]
ED50 0.0005In Vitro neurotrophic effect was measured in cultured chick DRG sensory neurons. [AID50622, Type: Literature]
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12
[SID103164548]
Kd 0.0005Binding affinity to purified elF4E [AID548276, Type: Literature]
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13
[SID103164548]
IC50 0.0006Compound was tested in vitro for its ability to compete with immobilized FK506 for binding to biotinylated FK506 binding protein 12 in a competitive binding assay [AID69125, Type: Literature]
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14
[SID103164548]
IC50 0.001Inhibitory activity against human concanavalin-A proliferation assay [AID88934, Type: Literature]
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15
[SID103164548]
IC50 0.001Compound was tested in vitro for its ability to inhibit the proliferation of the IL-6-dependent hybridoma clone B13-29-15 [AID93824, Type: Literature]
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16
[SID103164548]
IC50 0.001Compound was tested in vitro for inhibitory activity in the mixed lymphocyte reaction (MLR) assay [AID106878, Type: Literature]
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17
[SID103164548]
IC50 0.001In vitro immunosuppressive activity by splenocyte mitogenesis assay in spleen cells from BDF1 female mice at 1 pM to 10 uM concentration [AID132664, Type: other]
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18
[SID103164548]
IC50 0.001SANGER: Inhibition of human MFE-296 cell growth in a cell viability assay [AID485251, Type: other]
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19
[SID103164548]
EC50 0.0013Antiviral activity against HIV1 X4 assessed as inhibition of cell-cell fusion between X4-envelope expressing HEK293T cells and CD8 depleted human PBMCs pretreated for 6 days [AID406212, Type: Literature]
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20
[SID103164548]
IC50 0.0016The compound was tested for binding afifnity to FK506 binding protein 12 with an ascomycin conjugate of alkaline phosphatase in a competition binding assay [AID69247, Type: Literature]
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21
[SID103164548]
IC50 0.0016T-cell antiproliferative activity in human mixed lymphocyte reaction [AID257582, Type: Literature]
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22
[SID103164548]
IC50 0.0016Inhibitory activity against FKBP12 [AID257581, Type: Literature]Serine/threonine-protein kinase mTOR [gi:1169735]
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23
[SID103164548]
IC50 0.0016Inhibitory activity against FKBP12 [AID257581, Type: Literature]Serine/threonine-protein kinase mTOR [gi:1169735]
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24
[SID144206303]
Potency 0.0024qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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25
[SID144206303]
Potency 0.0024qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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26
[SID144206303]
Potency 0.0024qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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27
[SID103164548]
EC50 0.0025Antiviral activity against HIV1 X4 in human PBMC assessed as reduction of p24 antigen levels [AID406217, Type: Literature]
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28
[SID103164548]
IC50 0.003In vitro ability to inhibit lymphoproliferation (LAF) in vitro using cells from the thymus of normal BALB/c mice [AID132662, Type: Literature]
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29
[SID144206303]
Potency 0.0047qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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30
[SID144206303]
Potency 0.0047qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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31
[SID144206303]
Potency 0.0047qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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32
[SID144204421]
Potency 0.0084qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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33
[SID144204421]
Potency 0.0084qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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34
[SID144204421]
Potency 0.0084qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT [AID686978, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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35
[SID103164548]
IC50 0.009SANGER: Inhibition of human HO-1-N-1 cell growth in a cell viability assay [AID485066, Type: other]
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36
[SID103164548]
IC50 0.0098Tested for inhibition of T cell proliferation in the co-mitogen stimulated proliferation assay [AID209808, Type: other]
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37
[SID103164548]
IC50 0.01Inhibition of mTOR-mediated S6 phosphorylation in human PC3 cells [AID643753, Type: Literature]Serine/threonine-protein kinase mTOR [gi:1169735]
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38
[SID103164548]
IC50 0.01Inhibition of mTOR-mediated S6 phosphorylation in human PC3 cells [AID643753, Type: Literature]Serine/threonine-protein kinase mTOR [gi:1169735]
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39
[SID103164548]
IC50 0.01Antiproliferative activity against human PC3 cells [AID643755, Type: Literature]
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40
[SID144204421]
Potency 0.0119qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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41
[SID144204421]
Potency 0.0119qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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42
[SID144204421]
Potency 0.0119qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT [AID686979, Type: confirmatory]TDP1 protein [Homo sapiens] [gi:79154014]
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43
[SID103164548]
IC50 0.015Ability to bind to FK506 binding protein via its inhibition of peptidyl prolyl cis-trans isomerase activity (PPIase) inherent to FKBP [AID69092, Type: Literature]
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44
[SID103164548]
IC50 0.015SANGER: Inhibition of human CAL-39 cell growth in a cell viability assay [AID485079, Type: other]
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45
[SID103164548]
IC50 0.023SANGER: Inhibition of human CHL-1 cell growth in a cell viability assay [AID485072, Type: other]
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46
[SID103164548]
IC50 0.027SANGER: Inhibition of human Daoy cell growth in a cell viability assay [AID485129, Type: other]
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47
[SID103164548]
IC50 0.038SANGER: Inhibition of human UACC-893 cell growth in a cell viability assay [AID485268, Type: other]
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48
[SID103164548]
EC50 0.05Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay [AID601333, Type: Literature]
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49
[SID103164548]
IC50 0.082SANGER: Inhibition of human HN cell growth in a cell viability assay [AID485166, Type: other]
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50
[SID103164548]
IC50 0.088SANGER: Inhibition of human Detroit562 cell growth in a cell viability assay [AID485101, Type: other]
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