tofacitinib (CID 9926791) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(139)
 
 
Inactive(19)
 
 
Inconclusive(1)
 
 
Unspecified(854)
 
 
Top Targets:
PKc(96)
 
 
PKc like(60)
 
 
 
 
STKc AGC(48)
 
 
 
 
PTKc Abl(25)
 
 
 
PTKc EGFR(22)
 
 
BioAssay Types:
Literature(991)
 
 
 
 
Confirmatory(21)
 
 
 
 
BioActivity Types:
Kd(774)
 
 
 
IC50(90)
 
 
 
Potency(9)
 
 
 
Ki(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1001    Data Row: 1013   Total Pages: 21   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103506979]
Kd 0.00016Binding constant for JAK3(JH1domain-catalytic) kinase domain [AID624785, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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2
[SID103506979]
Kd 0.00016Binding constant for JAK3(JH1domain-catalytic) kinase domain [AID624785, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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3
[SID103506979]
Kd 0.00058Binding constant for JAK2(JH1domain-catalytic) kinase domain [AID624973, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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4
[SID103506979]
Kd 0.00058Binding constant for JAK2(JH1domain-catalytic) kinase domain [AID624973, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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5
[SID103506979]
Kd 0.00058Binding constant for JAK2(JH1domain-catalytic) kinase domain [AID624973, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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6
[SID103506979]
IC50 0.0006Inhibition of human recombinant N-terminal GST-tagged JAK3 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642231, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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7
[SID103506979]
IC50 0.0006Inhibition of human recombinant N-terminal GST-tagged JAK3 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642231, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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8
[SID103506979]
IC50 0.001Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA [AID547402, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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9
[SID103506979]
IC50 0.001Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA [AID547402, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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10
[SID103506979]
IC50 0.001Inhibition of JAK3 [AID413567, Type: Literature]
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11
[SID103506979]
IC50 0.001Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA [AID394064, Type: Literature]
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12
[SID103506979]
Ki 0.001Inhibition of JAK3 [AID512561, Type: Literature]
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13
[SID103506979]
IC50 0.0016Inhibition of JAK2 by solution phase kinase assay [AID547409, Type: Literature]
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14
[SID103506979]
Kd 0.0016Binding constant for JAK1(JH1domain-catalytic) kinase domain [AID624859, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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15
[SID103506979]
Kd 0.0016Binding constant for JAK1(JH1domain-catalytic) kinase domain [AID624859, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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16
[SID103506979]
Kd 0.0022Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435674, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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17
[SID103506979]
Kd 0.0022Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435674, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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18
[SID103506979]
Kd 0.0022Binding affinity to JAK3 [AID538230, Type: Literature]
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19
[SID103506979]
IC50 0.003Inhibition of human recombinant N-terminal GST-tagged JAK1 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642230, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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20
[SID103506979]
IC50 0.003Inhibition of human recombinant N-terminal GST-tagged JAK1 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642230, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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21
[SID103506979]
IC50 0.0032Inhibition of JAK3 by solution phase kinase assay [AID547408, Type: Literature]
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22
[SID103506979]
IC50 0.004Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642229, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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23
[SID103506979]
IC50 0.004Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642229, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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24
[SID103506979]
IC50 0.004Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642229, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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25
[SID103506979]
IC50 0.0041Inhibition of JAK1 by solution phase kinase assay [AID547410, Type: Literature]
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26
[SID103506979]
Kd 0.0045Binding affinity to DCamkL3 [AID413573, Type: Literature]
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27
[SID103506979]
Kd 0.0045Binding constant for DCAMKL3 kinase domain [AID435399, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
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28
[SID103506979]
Kd 0.0045Binding constant for DCAMKL3 kinase domain [AID435399, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
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29
[SID103506979]
Kd 0.0048Binding constant for TYK2(JH1domain-catalytic) kinase domain [AID624912, Type: Literature]Non-receptor tyrosine-protein kinase TYK [gi:56405328]
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30
[SID103506979]
Kd 0.0048Binding constant for TYK2(JH1domain-catalytic) kinase domain [AID624912, Type: Literature]Non-receptor tyrosine-protein kinase TYK [gi:56405328]
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31
[SID103506979]
Kd 0.0048Binding constant for TYK2(JH1domain-catalytic) kinase domain [AID624912, Type: Literature]Non-receptor tyrosine-protein kinase TYK [gi:56405328]
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32
[SID103506979]
Kd 0.005Binding affinity to JAK2 [AID538229, Type: Literature]
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33
[SID103506979]
IC50 0.005Inhibition of GST-tagged JAK3 kinase [AID468616, Type: Literature]
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34
[SID103506979]
Kd 0.005Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435658, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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35
[SID103506979]
Kd 0.005Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435658, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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36
[SID103506979]
Kd 0.005Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435658, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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37
[SID103506979]
IC50 0.0061Inhibition of GST-tagged Jak1 expressed in insect cells using 70 uM ATP [AID553350, Type: Literature]
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38
[SID103506979]
IC50 0.008Inhibition of GST-tagged Jak3 expressed in insect cells using 18 uM ATP [AID553352, Type: Literature]
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39
[SID103506979]
IC50 0.011Inhibition of human IL2-dependent T cell blast proliferation assessed as reduction in [3H]thymidine incorporation after 72 hrs post dose IL2 blast assay [AID547406, Type: Literature]
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40
[SID103506979]
IC50 0.011Inhibition of JAK2 by kinase-Glo luminescent assay [AID298727, Type: Literature]
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41
[SID103506979]
IC50 0.011Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting [AID393837, Type: Literature]
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42
[SID103506979]
IC50 0.011Inhibition of JAK2 [AID276240, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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43
[SID103506979]
IC50 0.011Inhibition of JAK2 [AID276240, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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44
[SID103506979]
IC50 0.011Inhibition of JAK2 [AID276240, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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45
[SID103506979]
IC50 0.012Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP [AID553351, Type: Literature]
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46
[SID103506979]
Kd 0.012Binding constant for DCAMKL3 kinase domain [AID624707, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
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47
[SID103506979]
Kd 0.012Binding constant for DCAMKL3 kinase domain [AID624707, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
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48
[SID103506979]
IC50 0.013Inhibition of JAK3 by kinase-Glo luminescent assay [AID298726, Type: Literature]
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49
[SID103506979]
IC50 0.013Inhibition of JAK3 [AID276239, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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50
[SID103506979]
IC50 0.013Inhibition of JAK3 [AID276239, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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