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INCB018424 (CID 25126798) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(160)
 
 
Inactive(14)
 
 
Unspecified(304)
 
 
Top Targets:
PKc(48)
 
 
 
PKc like(40)
 
 
 
STKc AGC(17)
 
 
 
PTKc Abl(16)
 
 
 
PTKc EGFR(12)
 
 
BioAssay Types:
Literature(463)
 
 
 
Confirmatory(15)
 
 
 
BioActivity Types:
Kd(442)
 
 
 
Potency(16)
 
 
 
IC50(10)
 
 
Ki(8)
 
 
EC50(2)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 478    Data Row: 478   Total Pages: 10   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID134449640]
Kd 3.6e-05Binding constant for JAK2(JH1domain-catalytic) kinase domain [AID624973, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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2
[SID134449640]
Ki 9e-05Inhibition of purified JAK1 incubated for 30 mins [AID706305, Type: Literature]
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3
[SID134449640]
Ki 0.0001Inhibition of JAK2 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins [AID696136, Type: Literature]
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4
[SID134449640]
Ki 0.0002Inhibition of JAK1 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins [AID696135, Type: Literature]
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5
[SID134449640]
Ki 0.00024Inhibition of purified JAK2 incubated for 30 mins [AID706320, Type: Literature]
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6
[SID134449640]
Ki 0.0005Inhibition of TYK2 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins [AID696138, Type: Literature]
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7
[SID134449640]
Ki 0.00055Inhibition of purified TYK2 incubated for 30 mins [AID706303, Type: Literature]
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8
[SID134449640]
Kd 0.0009Binding constant for TYK2(JH1domain-catalytic) kinase domain [AID624912, Type: Literature]Non-receptor tyrosine-protein kinase TYK2 [gi:56405328]
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9
[SID134449640]
IC50 0.00184Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation [AID706322, Type: Literature]
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10
[SID134449640]
Kd 0.002Binding constant for JAK3(JH1domain-catalytic) kinase domain [AID624785, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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11
[SID134449640]
IC50 0.0028Inhibition of human JAK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay [AID690495, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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12
[SID134449640]
IC50 0.003Inhibition of human recombinant JAK2 by TR-FRET assay [AID538224, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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13
[SID134449640]
IC50 0.003Inhibition of human recombinant JAK1 by TR-FRET assay [AID538223, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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14
[SID134449640]
Ki 0.0032Inhibition of JAK3 kinase domain using N-terminal 5-carboxyfluorescein-tagged Leu-Pro-Leu-Asp-Lys-Asp-Tyr-Tyr-Val-Val-Arg as substrate after 30 mins [AID696137, Type: Literature]
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15
[SID134449640]
Ki 0.00322Inhibition of purified JAK3 incubated for 30 mins [AID706304, Type: Literature]
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16
[SID134449640]
IC50 0.0033Inhibition of human JAK1 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay [AID690497, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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17
[SID134449640]
Kd 0.0034Binding constant for JAK1(JH1domain-catalytic) kinase domain [AID624859, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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18
[SID134449640]
IC50 0.00685Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO [AID706327, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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19
[SID134449640]
EC50 0.012Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measured after 30 to 45 mins [AID696140, Type: Literature]Tyrosine-protein kinase JAK2 [gi:12643404]
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20
[SID134449640]
IC50 0.019Inhibition of human TYK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay [AID690501, Type: Literature]Non-receptor tyrosine-protein kinase TYK2 [gi:56405328]
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21
[SID134449640]
IC50 0.019Inhibition of human recombinant TYK2 by TR-FRET assay [AID538226, Type: Literature]Non-receptor tyrosine-protein kinase TYK2 [gi:56405328]
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22
[SID134449640]
EC50 0.024Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins [AID696139, Type: Literature]Tyrosine-protein kinase JAK1 [gi:215274013]
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23
[SID134449640]
Kd 0.041Binding constant for MAP3K2 kinase domain [AID625062, Type: Literature]Mitogen-activated protein kinase kinase kinase 2 [gi:97536681]
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24
[SID134449640]
Kd 0.046Binding constant for CAMK2A kinase domain [AID624730, Type: Literature]Calcium/calmodulin-dependent protein kinase type II subunit alpha [gi:296434552]
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25
[SID134449640]
Kd 0.052Binding constant for ROCK2 kinase domain [AID624969, Type: Literature]Rho-associated protein kinase 2 [gi:269849761]
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26
[SID134449640]
Kd 0.06Binding constant for ROCK1 kinase domain [AID625015, Type: Literature]Rho-associated protein kinase 1 [gi:47605999]
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27
[SID134449640]
Kd 0.068Binding constant for DCAMKL1 kinase domain [AID624966, Type: Literature]Serine/threonine-protein kinase DCLK1 [gi:6225242]
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28
[SID134449640]
Kd 0.072Binding constant for DAPK1 kinase domain [AID624971, Type: Literature]Death-associated protein kinase 1 [gi:317373595]
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29
[SID134449640]
Kd 0.089Binding constant for DAPK3 kinase domain [AID624834, Type: Literature]Death-associated protein kinase 3 [gi:38604691]
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30
[SID134449640]
Kd 0.09Binding constant for LRRK2(G2019S) kinase domain [AID624741, Type: Literature]Leucine-rich repeat serine/threonine-protein kinase 2 [gi:294862450]
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31
[SID134449640]
Kd 0.09Binding constant for CAMK2D kinase domain [AID624770, Type: Literature]Calcium/calmodulin-dependent protein kinase type II subunit delta [gi:116242602]
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32
[SID134449640]
Kd 0.097Binding constant for DAPK2 kinase domain [AID625077, Type: Literature]Death-associated protein kinase 2 [gi:38605084]
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33
[SID134449640]
Kd 0.099Binding constant for GAK kinase domain [AID625012, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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34
[SID134449640]
Kd 0.1Binding constant for CAMK2G kinase domain [AID624731, Type: Literature]Calcium/calmodulin-dependent protein kinase type II subunit gamma [gi:62512173]
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35
[SID134449640]
Kd 0.12Binding constant for CAMK1D kinase domain [AID625118, Type: Literature]Calcium/calmodulin-dependent protein kinase type 1D [gi:56404610]
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36
[SID134449640]
Kd 0.12Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain [AID624901, Type: Literature]Ribosomal protein S6 kinase alpha-1 [gi:20178306]
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37
[SID134449640]
Kd 0.12Binding constant for AAK1 kinase domain [AID625089, Type: Literature]AP2-associated protein kinase 1 [gi:300669613]
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38
[SID134449640]
Kd 0.13Binding constant for PLK1 kinase domain [AID624975, Type: Literature]Serine/threonine-protein kinase PLK1 [gi:1709658]
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39
[SID134449640]
Kd 0.14Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain [AID624967, Type: Literature]Ribosomal protein S6 kinase alpha-5 [gi:37999482]
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40
[SID134449640]
Kd 0.15Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain [AID625082, Type: Literature]Ribosomal protein S6 kinase alpha-6 [gi:11133131]
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41
[SID134449640]
Kd 0.15Binding constant for MAP3K3 kinase domain [AID624865, Type: Literature]Mitogen-activated protein kinase kinase kinase 3 [gi:160332306]
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42
[SID134449640]
Kd 0.15Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain [AID624805, Type: Literature]Ribosomal protein S6 kinase alpha-2 [gi:90110031]
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43
[SID134449640]
Kd 0.19Binding constant for ULK2 kinase domain [AID625085, Type: Literature]Serine/threonine-protein kinase ULK2 [gi:296453001]
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44
[SID134449640]
Kd 0.19Binding constant for RET(V804M) kinase domain [AID625124, Type: Literature]Proto-oncogene tyrosine-protein kinase receptor Ret [gi:547807]
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45
[SID134449640]
Kd 0.2Binding constant for MKNK2 kinase domain [AID625108, Type: Literature]MAP kinase-interacting serine/threonine-protein kinase 2 [gi:90102033]
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46
[SID134449640]
Kd 0.2Binding constant for PLK4 kinase domain [AID625076, Type: Literature]Serine/threonine-protein kinase PLK4 [gi:160113150]
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47
[SID134449640]
Kd 0.21Binding constant for BIKE kinase domain [AID625109, Type: Literature]BMP-2-inducible protein kinase [gi:34222653]
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48
[SID134449640]
Kd 0.26Binding constant for DCAMKL3 kinase domain [AID624707, Type: Literature]Serine/threonine-protein kinase DCLK3 [gi:115502142]
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49
[SID134449640]
Kd 0.27Binding constant for YSK4 kinase domain [AID625136, Type: Literature]Mitogen-activated protein kinase kinase kinase 19 [gi:74755104]
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50
[SID134449640]
Kd 0.28Binding constant for RET(V804L) kinase domain [AID625123, Type: Literature]Proto-oncogene tyrosine-protein kinase receptor Ret [gi:547807]
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