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tofacitinib (CID 9926791) - Compound BioActivity Data
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BioActivity Outcomes:
Active(208)
 
 
Inactive(35)
 
 
Inconclusive(1)
 
 
Unspecified(877)
 
 
Top Targets:
PKc(85)
 
 
PKc like(65)
 
 
 
 
PTKc Jak2 Jak..(48)
 
 
 
STKc AGC(33)
 
 
 
 
PTKc Jak1 rpt..(24)
 
 
 
BioAssay Types:
Literature(1088)
 
 
 
 
Confirmatory(31)
 
 
 
 
BioActivity Types:
Kd(774)
 
 
 
IC50(135)
 
 
 
Potency(21)
 
 
 
 
Ki(13)
 
 
EC50(10)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1102    Data Row: 1121   Total Pages: 57   Display: Page     
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#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]
Ki 0.00024Inhibition of human recombinant JAK3 kinase domain using FITC-KGGEEEEYFELVKK as substrate by peptide mobility shift assay [AID690498, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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3
[SID103506979]
Ki 0.0004Inhibition of JAK3 (unknown origin) using Leu-Pro-Leu-Asp-Lys-Asp-Tyr-Tyr-Val-Val-Arg as substrate after 30 mins in presence of ATP [AID750409, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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4
[SID103506979]
Ki 0.0004Inhibition of human GST-fused JAK3 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA [AID750601, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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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]
Ki 0.00068Inhibition of human recombinant GST-tagged JAK1 using 5-FAM-KKSRGDYMTMQIG as substrate by peptide mobility shift assay [AID690500, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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8
[SID103506979]
Ki 0.0007Inhibition of recombinant JAK1 (unknown origin) using Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins in presence of ATP [AID750444, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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9
[SID103506979]
Ki 0.0007Inhibition of human GST-fused JAK1 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA [AID750603, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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10
[SID103506979]
Ki 0.0007Inhibition of recombinant JAK2 (unknown origin) using Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins in presence of ATP [AID750445, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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11
[SID103506979]
Ki 0.0007Inhibition of human GST-fused JAK2 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA [AID750602, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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12
[SID103506979]
Ki 0.00099Inhibition of human recombinant JAK2 kinase domain using FITC-KGGEEEEYFELVKK as substrate by peptide mobility shift assay [AID690499, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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13
[SID103506979]
Ki 0.001Inhibition of JAK3 [AID512561, Type: Literature]
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14
[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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15
[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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16
[SID103506979]
IC50 0.001Inhibition of JAK3 [AID413567, Type: Literature]
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17
[SID103506979]
IC50 0.0014Inhibition of JAK3 (unknown origin) [AID1070026, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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18
[SID103506979]
IC50 0.0016Inhibition of JAK2 by solution phase kinase assay [AID547409, Type: Literature]
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19
[SID103506979]
IC50 0.0016Inhibition of JAK1 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 1 hr by scintillation counting analysis in presence of [gamma-33P]ATP [AID726696, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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20
[SID170482324]
IC50 0.0016Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB [AID977608, Type: Literature]Chain A, Crystal Structures Of Jak1 And Jak2 Inhibitor Complexes [gi:222447066]
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