Bookmark and Share
tofacitinib (CID 9926791) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(165)
 
 
Inactive(26)
 
 
Inconclusive(1)
 
 
Unspecified(860)
 
 
Top Targets:
PKc(85)
 
 
PKc like(65)
 
 
 
 
STKc AGC(33)
 
 
 
 
PTKc Jak2 Jak..(26)
 
 
 
PTKc Abl(24)
 
 
 
BioAssay Types:
Literature(1023)
 
 
 
 
Confirmatory(28)
 
 
 
 
BioActivity Types:
Kd(774)
 
 
 
IC50(107)
 
 
 
Potency(17)
 
 
 
 
Ki(5)
 
 
EC50(3)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1040    Data Row: 1052   Total Pages: 22   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]
View
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]
View
3
[SID103506979]
Kd 0.00058Binding constant for JAK2(JH1domain-catalytic) kinase domain [AID624973, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
View
4
[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]
View
5
[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]
View
6
[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]
View
7
[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]
View
8
[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]
View
9
[SID103506979]
IC50 0.001Inhibition of JAK3 [AID413567, Type: Literature]
View
10
[SID103506979]
Ki 0.001Inhibition of JAK3 [AID512561, Type: Literature]
View
11
[SID103506979]
IC50 0.0016Inhibition of JAK2 by solution phase kinase assay [AID547409, Type: Literature]
View
12
[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]
View
13
[SID103506979]
Kd 0.0016Binding constant for JAK1(JH1domain-catalytic) kinase domain [AID624859, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
View
14
[SID103506979]
Kd 0.0022Binding affinity to JAK3 [AID538230, Type: Literature]
View
15
[SID103506979]
IC50 0.0022Inhibition of JAK3 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP [AID726698, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
View
16
[SID103506979]
Kd 0.0022Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435674, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
View
17
[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]
View
18
[SID103506979]
IC50 0.0032Inhibition of JAK3 by solution phase kinase assay [AID547408, Type: Literature]
View
19
[SID103506979]
IC50 0.004Inhibition of JAK2 (unknown origin)-mediated phosphorylation of Biotin-KAIETDKEYYTVKD incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]ATP [AID726697, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
View
20
[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]
View
21
[SID103506979]
IC50 0.0041Inhibition of JAK1 by solution phase kinase assay [AID547410, Type: Literature]
View
22
[SID103506979]
Ki 0.00439Inhibition of human recombinant GST-tagged TYK2 using 5-FAM-KKSRGDYMTMQIG as substrate by peptide mobility shift assay [AID690496, Type: Literature]Non-receptor tyrosine-protein kinase TYK2 [gi:56405328]
View
23
[SID103506979]
Kd 0.0045Binding constant for DCAMKL3 kinase domain [AID435399, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
View
24
[SID103506979]
Kd 0.0045Binding affinity to DCamkL3 [AID413573, Type: Literature]
View
25
[SID103506979]
Kd 0.0048Binding constant for TYK2(JH1domain-catalytic) kinase domain [AID624912, Type: Literature]Non-receptor tyrosine-protein kinase TYK2 [gi:56405328]
View
26
[SID103506979]
IC50 0.005Inhibition of GST-tagged JAK3 kinase [AID468616, Type: Literature]
View
27
[SID103506979]
Kd 0.005Binding affinity to JAK2 [AID538229, Type: Literature]
View
28
[SID103506979]
Kd 0.005Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435658, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
View
29
[SID103506979]
IC50 0.0061Inhibition of GST-tagged Jak1 expressed in insect cells using 70 uM ATP [AID553350, Type: Literature]
View
30
[SID103506979]
IC50 0.008Inhibition of GST-tagged Jak3 expressed in insect cells using 18 uM ATP [AID553352, Type: Literature]
View
31
[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]
View
32
[SID103506979]
IC50 0.011Inhibition of JAK2 by kinase-Glo luminescent assay [AID298727, Type: Literature]
View
33
[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]
View
34
[SID103506979]
IC50 0.011Inhibition of JAK2 [AID276240, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
View
35
[SID103506979]
IC50 0.012Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP [AID553351, Type: Literature]
View
36
[SID103506979]
Kd 0.012Binding constant for DCAMKL3 kinase domain [AID624707, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
View
37
[SID103506979]
IC50 0.013Inhibition of JAK3 by kinase-Glo luminescent assay [AID298726, Type: Literature]
View
38
[SID103506979]
IC50 0.013Inhibition of JAK3 [AID276239, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
View
39
[SID103506979]
IC50 0.02Inhibition of JAK2 [AID413568, Type: Literature]
View
40
[SID103506979]
IC50 0.02Inhibition of JAK2 [AID394055, Type: Literature]
View
41
[SID103506979]
IC50 0.024Inhibition of Jak3-mediated IL15-induced Stat5 phosphorylation in human MO7 cells by cell-based assay [AID553355, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
View
42
[SID103506979]
IC50 0.026Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay [AID642237, Type: Literature]
View
43
[SID103506979]
IC50 0.028Inhibition of JAK3/JAK1 in human PBMC expressing CD3 assessed as inhibition of IL-2-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis [AID726525, Type: Literature]
View
44
[SID103506979]
IC50 0.033Inhibition of JAK1/JAK3 in human PBMC assessed as inhibition of IL2-stimulated STATs phosphorylation preincubated for 30 mins prior to IL2 challenge measured after 15 mins by intracellular phosflow staining [AID642305, Type: Literature]
View
45
[SID103506979]
IC50 0.033Inhibition of GST-tagged JAK2 kinase [AID468614, Type: Literature]
View
46
[SID103506979]
IC50 0.034Inhibition of Tyk2 by solution phase kinase assay [AID549358, Type: Literature]
View
47
[SID103506979]
IC50 0.048Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay [AID553354, Type: Literature]Tyrosine-protein kinase JAK3 [gi:156630890]
View
48
[SID103506979]
IC50 0.05Inhibition of JAK3/JAK1 in C57BL/6 mouse whole blood assessed as inhibition of IL-2-stimulated STAT5a phosphorylation after 30 mins by flow cytometric analysis [AID726502, Type: Literature]
View
49
[SID103506979]
IC50 0.052Inhibition of human recombinant N-terminal GST-tagged TYK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay [AID642232, Type: Literature]Non-receptor tyrosine-protein kinase TYK2 [gi:56405328]
View
50
[SID103506979]
EC50 0.053Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL2-induced STAT3 phosphorylation [AID690507, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
View