4-methyl-N-(3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-pyridin-3-ylpyrimidin-2-yl)amino)benzamide (CID 644241) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(116)
 
 
Inactive(24)
 
 
Inconclusive(3)
 
 
Unspecified(367)
 
 
Top Targets:
PKc(55)
 
 
PKc like(34)
 
 
 
STKc AGC(24)
 
 
PTKc Abl(17)
 
 
 
PTKc EGFR(12)
 
 
BioAssay Types:
Literature(484)
 
 
 
 
Confirmatory(12)
 
 
 
 
Screening(11)
 
 
BioActivity Types:
Kd(442)
 
 
 
IC50(35)
 
 
 
Potency(12)
 
 
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 508    Data Row: 510   Total Pages: 11   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103563888]
Kd 0.0011Binding constant for DDR1 kinase domain [AID624850, Type: Literature]Epithelial discoidin domain-containing receptor 1 [gi:729008]
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2
[SID103563888]
Kd 0.0011Binding constant for DDR1 kinase domain [AID624850, Type: Literature]Epithelial discoidin domain-containing receptor 1 [gi:729008]
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3
[SID103563888]
IC50 0.0034Antiproliferative activity against human KU812 cells [AID590030, Type: Literature]
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4
[SID103563888]
IC50 0.0037Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA [AID515827, Type: Literature]
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5
[SID103563888]
Kd 0.0049Binding constant for ABL1(H396P)-nonphosphorylated kinase domain [AID624983, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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6
[SID103563888]
Kd 0.0049Binding constant for ABL1(H396P)-nonphosphorylated kinase domain [AID624983, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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7
[SID103563888]
IC50 0.0052Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA [AID515826, Type: Literature]
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8
[SID103563888]
IC50 0.0065Antiproliferative activity against human K562 cells [AID590029, Type: Literature]
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9
[SID103563888]
Kd 0.01Binding constant for ABL1-nonphosphorylated kinase domain [AID624991, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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10
[SID103563888]
Kd 0.01Binding constant for ABL1-nonphosphorylated kinase domain [AID624991, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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11
[SID103563888]
Kd 0.01Binding constant for ABL1(Q252H)-nonphosphorylated kinase domain [AID624986, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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12
[SID103563888]
Kd 0.01Binding constant for ABL1(Q252H)-nonphosphorylated kinase domain [AID624986, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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13
[SID103563888]
Kd 0.011Binding constant for ZAK kinase domain [AID624755, Type: Literature]Mitogen-activated protein kinase kinase kinase MLT [gi:313104215]
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14
[SID103563888]
Kd 0.011Binding constant for ZAK kinase domain [AID624755, Type: Literature]Mitogen-activated protein kinase kinase kinase MLT [gi:313104215]
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15
[SID103563888]
Kd 0.012Binding constant for ABL1(F317L)-nonphosphorylated kinase domain [AID624981, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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16
[SID103563888]
Kd 0.012Binding constant for ABL1(F317L)-nonphosphorylated kinase domain [AID624981, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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17
[SID103563888]
Kd 0.013Binding constant for ABL1-phosphorylated kinase domain [AID624992, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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18
[SID103563888]
Kd 0.013Binding constant for ABL1-phosphorylated kinase domain [AID624992, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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19
[SID103563888]
Kd 0.013Binding constant for ABL1(Y253F)-phosphorylated kinase domain [AID624990, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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20
[SID103563888]
Kd 0.013Binding constant for ABL1(Y253F)-phosphorylated kinase domain [AID624990, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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21
[SID103563888]
Kd 0.014Binding constant for ABL1(F317L)-phosphorylated kinase domain [AID624982, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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22
[SID103563888]
Kd 0.014Binding constant for ABL1(F317L)-phosphorylated kinase domain [AID624982, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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23
[SID103563888]
Kd 0.015Binding constant for ABL1(M351T)-phosphorylated kinase domain [AID624985, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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24
[SID103563888]
Kd 0.015Binding constant for ABL1(M351T)-phosphorylated kinase domain [AID624985, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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25
[SID103563888]
Kd 0.018Binding constant for ABL1(F317I)-nonphosphorylated kinase domain [AID624979, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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26
[SID103563888]
Kd 0.018Binding constant for ABL1(F317I)-nonphosphorylated kinase domain [AID624979, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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27
[SID103563888]
IC50 0.02Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells [AID515831, Type: Literature]
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28
[SID103563888]
IC50 0.021Antiproliferative activity against human K562 cells [AID515834, Type: Literature]
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29
[SID103563888]
Kd 0.021Binding constant for ABL1(H396P)-phosphorylated kinase domain [AID624984, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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30
[SID103563888]
Kd 0.021Binding constant for ABL1(H396P)-phosphorylated kinase domain [AID624984, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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31
[SID103563888]
Kd 0.021Binding constant for ABL1(Q252H)-phosphorylated kinase domain [AID624987, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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32
[SID103563888]
Kd 0.021Binding constant for ABL1(Q252H)-phosphorylated kinase domain [AID624987, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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33
[SID103563888]
Kd 0.022Binding constant for KIT(L576P) kinase domain [AID624790, Type: Literature]Mast/stem cell growth factor receptor Kit [gi:125472]
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34
[SID103563888]
Kd 0.022Binding constant for KIT(L576P) kinase domain [AID624790, Type: Literature]Mast/stem cell growth factor receptor Kit [gi:125472]
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35
[SID103563888]
IC50 0.025Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells [AID515835, Type: Literature]
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36
[SID103563888]
IC50 0.025Inhibition of PDGFR [AID463623, Type: Literature]
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37
[SID103563888]
Kd 0.026Binding constant for ABL2 kinase domain [AID624993, Type: Literature]Abelson tyrosine-protein kinase 2 [gi:1168268]
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38
[SID103563888]
Kd 0.026Binding constant for ABL2 kinase domain [AID624993, Type: Literature]Abelson tyrosine-protein kinase 2 [gi:1168268]
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39
[SID103563888]
Kd 0.029Binding constant for KIT kinase domain [AID624786, Type: Literature]Mast/stem cell growth factor receptor Kit [gi:125472]
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40
[SID103563888]
Kd 0.029Binding constant for KIT kinase domain [AID624786, Type: Literature]Mast/stem cell growth factor receptor Kit [gi:125472]
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41
[SID103563888]
Kd 0.033Binding constant for DDR2 kinase domain [AID624777, Type: Literature]Discoidin domain-containing receptor 2 [gi:215273969]
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42
[SID103563888]
Kd 0.033Binding constant for DDR2 kinase domain [AID624777, Type: Literature]Discoidin domain-containing receptor 2 [gi:215273969]
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43
[SID103563888]
Kd 0.036Binding constant for p38-beta kinase domain [AID624890, Type: Literature]Mitogen-activated protein kinase 11 [gi:134047835]
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44
[SID103563888]
Kd 0.036Binding constant for p38-beta kinase domain [AID624890, Type: Literature]Mitogen-activated protein kinase 11 [gi:134047835]
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45
[SID103563888]
Kd 0.036Binding constant for ABL1(E255K)-phosphorylated kinase domain [AID624978, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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46
[SID103563888]
Kd 0.036Binding constant for ABL1(E255K)-phosphorylated kinase domain [AID624978, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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47
[SID103563888]
Kd 0.037Binding constant for EPHA8 kinase domain [AID625120, Type: Literature]Ephrin type-A receptor 8 [gi:19857975]
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48
[SID103563888]
Kd 0.037Binding constant for EPHA8 kinase domain [AID625120, Type: Literature]Ephrin type-A receptor 8 [gi:19857975]
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49
[SID103563888]
IC50 0.038Inhibition of wild type Abl [AID463625, Type: Literature]
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50
[SID103563888]
IC50 0.0393Inhibition of Bcr/Abl by FRET-based Z-lyte assay [AID590028, Type: Literature]
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