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EKB 569 (CID 6445562) - Compound BioActivity Data
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BioActivity Outcomes:
Active(204)
 
 
Inactive(153)
 
 
Unspecified(227)
 
 
Top Targets:
PKc(52)
 
 
 
 
PKc like(49)
 
 
 
 
PTKc EGFR(31)
 
 
 
STKc AGC(29)
 
 
 
 
PTKc Abl(23)
 
 
 
BioAssay Types:
Literature(475)
 
 
 
 
Confirmatory(108)
 
 
 
BioActivity Types:
Kd(437)
 
 
 
 
IC50(23)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 476    Data Row: 584   Total Pages: 12   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103730344]
Kd 0.00023Binding constant for EGFR(L747-T751del,Sins) kinase domain [AID435906, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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2
[SID103730344]
IC50 0.00024Inhibition of EGFR [AID510254, Type: Literature]
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3
[SID103730344]
Kd 0.00024Binding constant for EGFR(G719C) kinase domain [AID435157, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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4
[SID103730344]
Kd 0.00024Binding constant for EGFR(L747-E749del, A750P) kinase domain [AID435652, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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5
[SID103730344]
Kd 0.00027Binding constant for EGFR(L747-S752del, P753S) kinase domain [AID435653, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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6
[SID103730344]
Kd 0.00033Binding constant for EGFR(S752-I759del) kinase domain [AID435792, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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7
[SID103730344]
Kd 0.00038Binding constant for EGFR(E746-A750del) kinase domain [AID435791, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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8
[SID103730344]
Kd 0.00041Binding constant for EGFR(L858R) kinase domain [AID435525, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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9
[SID103730344]
Kd 0.00042Binding constant for EGFR(G719S) kinase domain [AID435402, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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10
[SID103730344]
Kd 0.00044Binding constant for EGFR kinase domain [AID435156, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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11
[SID103730344]
Kd 0.00044Binding constant for EGFR(L861Q) kinase domain [AID435907, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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12
[SID103730344]
IC50 0.0006Inhibition of human EGFR in presence of 1 uM ATP [AID295762, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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13
[SID103730344]
Kd 0.001Average Binding Constant for EGFR ; NA=Not Active at 10 uM [AID256664, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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14
[SID103730344]
Kd 0.0015Average Binding Constant for GAK ; NA=Not Active at 10 uM [AID256612, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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15
[SID103730344]
Kd 0.0037Average Binding Constant for MAP4K5 ; NA=Not Active at 10 uM [AID256565, Type: Literature]Mitogen-activated protein kinase kinase kinase kinase 5 [gi:30316147]
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16
[SID103730344]
Kd 0.0064Binding constant for GAK kinase domain [AID435821, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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17
[SID103730344]
IC50 0.00802Inhibition of EGFR autophosphorylation in human A431 cells [AID510404, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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18
[SID103730344]
IC50 0.01Concentration required to inhibit growth of human carcinoma breast (SKBR3) cell line [AID202682, Type: Literature]
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19
[SID103730344]
IC50 0.01Inhibition of human A431 cell proliferation [AID247761, Type: Literature]
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20
[SID103730344]
Kd 0.01Binding constant for MAP4K5 kinase domain [AID435805, Type: Literature]Mitogen-activated protein kinase kinase kinase kinase 5 [gi:30316147]
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21
[SID103730344]
IC50 0.0145Inhibition of peptide substrate phosphorylation by epidermal growth factor receptor [AID66621, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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22
[SID103730344]
Kd 0.021Binding constant for ERBB4 kinase domain [AID435797, Type: Literature]Tubulin alpha-1A chain [gi:55977470]
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23
[SID103730344]
Kd 0.025Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain [AID435674, Type: Literature]Tyrosine-protein kinase JAK3 [gi:50403745]
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24
[SID103730344]
IC50 0.0349Inhibition of human EGFR in presence of 1 mM ATP [AID295765, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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25
[SID103730344]
IC50 0.0385Inhibition of human EGFR [AID362392, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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26
[SID103730344]
Kd 0.044Average Binding Constant for LCK ; NA=Not Active at 10 uM [AID256657, Type: Literature]Tyrosine-protein kinase Lck [gi:125474]
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27
[SID103730344]
Kd 0.045Average Binding Constant for TNIK ; NA=Not Active at 10 uM [AID256566, Type: Literature]TRAF2 and NCK-interacting protein kinase [gi:29840818]
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28
[SID103730344]
Kd 0.057Average Binding Constant for STK17A ; NA=Not Active at 10 uM [AID256568, Type: Literature]Serine/threonine-protein kinase 17A [gi:317373279]
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29
[SID103730344]
Kd 0.059Binding constant for DMPK kinase domain [AID435285, Type: Literature]Myotonin-protein kinase [gi:363548519]
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30
[SID103730344]
Kd 0.077Average Binding Constant for ERBB2 ; NA=Not Active at 10 uM [AID256662, Type: Literature]Receptor tyrosine-protein kinase erbB-2 [gi:119533]
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31
[SID103730344]
Kd 0.078Binding constant for BLK kinase domain [AID435646, Type: Literature]Tyrosine-protein kinase Blk [gi:158936749]
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32
[SID103730344]
IC50 0.07943Inhibition autophosphorylation of EGFR in human DiFi cells after 2 hrs by ELISA [AID603958, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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33
[SID103730344]
IC50 0.08Concentration required to inhibit autophosphorylation of cytoplasmic domain of epidermal growth factor receptor (EGFR) [AID69431, Type: Literature]
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34
[SID103730344]
IC50 0.08Inhibition of autophosphorylation of cytoplasmic domain of epidermal growth factor receptor [AID69432, Type: Literature]
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35
[SID103730344]
IC50 0.08Concentration required to inhibit growth of human carcinoma epidermoid (A431) cell line [AID7879, Type: Literature]
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36
[SID103730344]
IC50 0.08Inhibition of human epidermal growth factor receptor (EGFR) autophosphorylation [AID248903, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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37
[SID103730344]
IC50 0.083Inhibition of Epidermal Growth Factor Receptor (EGFR) autophosphorylation [AID69416, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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38
[SID103730344]
Kd 0.097Average Binding Constant for CSNK1E ; NA=Not Active at 10 uM [AID256644, Type: Literature]Casein kinase I isoform epsilon [gi:1346369]
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39
[SID103730344]
IC50 0.0976Inhibition of epidermal growth factor receptor kinase autophosphorylation [AID66620, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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40
[SID103730344]
Kd 0.099Binding constant for LCK kinase domain [AID435676, Type: Literature]Tyrosine-protein kinase Lck [gi:125474]
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41
[SID103730344]
Kd 0.1Binding constant for full-length CSNK1E [AID435650, Type: Literature]Casein kinase I isoform epsilon [gi:1346369]
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42
[SID103730344]
Kd 0.11Average Binding Constant for STK10 ; NA=Not Active at 10 uM [AID256604, Type: Literature]Serine/threonine-protein kinase 10 [gi:12643358]
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43
[SID103730344]
Kd 0.11Average Binding Constant for ABL1(Y253F) ; NA=Not Active at 10 uM [AID256671, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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44
[SID103730344]
Kd 0.12Average Binding Constant for SRC ; NA=Not Active at 10 uM [AID256676, Type: Literature]Proto-oncogene tyrosine-protein kinase Src [gi:125711]
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45
[SID103730344]
Kd 0.13Average Binding Constant for ABL1(M351T) ; NA=Not Active at 10 uM [AID256669, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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46
[SID103730344]
Kd 0.13Average Binding Constant for MAP3K4 ; NA=Not Active at 10 uM [AID256564, Type: Literature]Mitogen-activated protein kinase kinase kinase 4 [gi:296434576]
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47
[SID103730344]
Kd 0.14Average Binding Constant for NEK2 ; NA=Not Active at 10 uM [AID256593, Type: Literature]Serine/threonine-protein kinase Nek2 [gi:1709252]
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48
[SID103730344]
Kd 0.16Average Binding Constant for ABL2 ; NA=Not Active at 10 uM [AID256641, Type: Literature]Abelson tyrosine-protein kinase 2 [gi:1168268]
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49
[SID103730344]
Kd 0.16Average Binding Constant for ABL1(Q252H) ; NA=Not Active at 10 uM [AID256666, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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50
[SID103730344]
Kd 0.17Average Binding Constant for ABL1(H396P) ; NA=Not Active at 10 uM [AID256668, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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