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CHEMBL364623 (CID 11153014) - Compound BioActivity Data
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BioActivity Outcomes:
Active(33)
 
 
Unspecified(23)
 
 
Top Targets:
PTKc Src like(4)
 
 
PTKc Lck Blk(2)
 
 
PTKc Abl(1)
 
 
PTKc HER2(1)
 
 
RhoGAP Bcr(1)
 
 
BioAssay Types:
Literature(56)
 
 
 
BioActivity Types:
IC50(34)
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 55    Data Row: 56   Total Pages: 2   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103454583]
Ki 0.00013In vitro inhibitory activity against recombinant p56 lck tyrosine kinase expressed as a His-tagged protein in insect cells [AID239502, Type: Literature]
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2
[SID103454583]
IC50 0.0008Inhibition of Fgr [AID271956, Type: Literature]Tyrosine-protein kinase Fgr [gi:125358]
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3
[SID103454583]
IC50 0.001Inhibition of Fyn [AID271967, Type: Literature]Tyrosine-protein kinase Fyn [gi:125370]
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4
[SID103454583]
IC50 0.001Inhibition of human Lck in presence of ATP [AID271946, Type: Literature]Tyrosine-protein kinase Lck [gi:125474]
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5
[SID103454583]
IC50 0.001Inhibitory activity against Fgr kinase [AID240534, Type: Literature]
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6
[SID103454583]
IC50 0.001inhibitory activity against Fyn protein kinase [AID240651, Type: Literature]
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7
[SID103454583]
IC50 0.001Inhibitory activity against Lck tyrosine kinase [AID240659, Type: Literature]
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8
[SID103454583]
IC50 0.001Inhibitory activity against Src tyrosine kinase [AID240660, Type: Literature]
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9
[SID103454583]
IC50 0.001Inhibitory activity against B lymphoid tyrosine kinase [AID240817, Type: Literature]
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10
[SID103454583]
IC50 0.0012In vitro inhibitory activity against recombinant p56 lck tyrosine kinase expressed as a His-tagged protein in insect cells [AID242530, Type: Literature]
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11
[SID103454583]
IC50 0.0016Antiproliferative activity against human K562 cells after 72 hrs [AID282221, Type: Literature]
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12
[SID103454583]
IC50 0.002Inhibition of Src in presence of ATP [AID271950, Type: Literature]Proto-oncogene tyrosine-protein kinase Src [gi:125711]
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13
[SID103454583]
IC50 0.002Inhibition of Yes [AID271968, Type: Literature]Tyrosine-protein kinase Yes [gi:125870]
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14
[SID103454583]
IC50 0.002Inhibition of Hck [AID271955, Type: Literature]Tyrosine-protein kinase HCK [gi:20141296]
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15
[SID103454583]
IC50 0.002inhibitory activity against Hck kinase [AID240535, Type: Literature]
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16
[SID103454583]
IC50 0.003Inhibition of Bcr-Abl in presence of ATP [AID271951, Type: Literature]Tyrosine-protein kinase ABL1 [gi:85681908]
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17
[SID103454583]
IC50 0.003Inhibition of Bcr-Abl in presence of ATP [AID271951, Type: Literature]Breakpoint cluster region protein [gi:143811366]
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18
[SID103454583]
IC50 0.004Inhibition of Lyn [AID271969, Type: Literature]Tyrosine-protein kinase Lyn [gi:125480]
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19
[SID103454583]
IC50 0.006inhibitory activity against Janus kinase 3 [AID240595, Type: Literature]
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20
[SID103454583]
IC50 0.067Antiproliferative activity against human PC3 cells after 72 hrs [AID282222, Type: Literature]
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21
[SID103454583]
IC50 0.08In vivo inhibitory activity against proliferation of normal human peripheral blood T lymphocytes [AID248495, Type: Literature]
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22
[SID103454583]
IC50 0.08Inhibition of anti CD3/anti CD28-induced T cell proliferation [AID271947, Type: Literature]
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23
[SID103454583]
IC50 0.202Inhibition of p38 kinase [AID271954, Type: Literature]
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24
[SID103454583]
IC50 0.5Inhibition of Her2 [AID271972, Type: Literature]Receptor tyrosine-protein kinase erbB-2 [gi:119533]
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25
[SID103454583]
IC50 0.67Inhibition of LPS-induced TNFalpha production in human PBMC [AID271957, Type: Literature]
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26
[SID103454583]
IC50 5.2Inhibitory activity against HER2 kinase [AID240554, Type: Literature]
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27
[SID103454583]
IC50 5.2Inhibition of Her1 [AID271971, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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28
[SID103454583]
IC50 5.5In vitro inhibitory activity against recombinant p56 lck tyrosine kinase expressed as a His-tagged protein in insect cells in presence of 1 mM ATP [AID242723, Type: Literature]
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29
[SID103454583]
Cmax in rat at 10 mg/kg, iv and po [AID271958, Type: Literature]
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30
[SID103454583]
Maximum plasma concentration was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID236663, Type: Literature]
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31
[SID103454583]
IC50 Inhibition of murine Lck in presence of ATP [AID271945, Type: Literature]Proto-oncogene tyrosine-protein kinase LCK [gi:78099784]
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32
[SID103454583]
Reduction of Freund's adjuvant induced paw edema in Lewis rat at 0.3 mg/kg, po [AID271965, Type: Literature]
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33
[SID103454583]
Reduction of Freund's adjuvant- induced paw edema in Lewis rat at 3 mg/kg, po [AID271966, Type: Literature]
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34
[SID103454583]
IC50 10Inhibition of FGFR1 [AID271973, Type: Literature]Fibroblast growth factor receptor 1 [gi:120046]
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35
[SID103454583]
IC50 10Inhibitory activity against Fibroblast growth factor receptor 1 [AID241123, Type: Literature]
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36
[SID103454583]
IC50 10inhibitory activity against Vascular endothelial growth factor receptor 2 [AID241417, Type: Literature]
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37
[SID103454583]
IC50 25Inhibitory activity against Cyclin-dependent kinase 2 [AID240788, Type: Literature]
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38
[SID103454583]
IC50 25Inhibitory activity against Cyclin-dependent kinase 4 [AID240789, Type: Literature]
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39
[SID103454583]
IC50 25Inhibition of Cdk2 [AID271970, Type: Literature]Cyclin-dependent kinase 2 [gi:116051]
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40
[SID103454583]
Time required to reach the maximum plasma concentration was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID236991, Type: Literature]
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41
[SID103454583]
Half-life was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID237159, Type: Literature]
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42
[SID103454583]
Oral bioavailability was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID236044, Type: Literature]
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43
[SID103454583]
Plasma clearance was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID236244, Type: Literature]
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44
[SID103454583]
Mean residence time was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID236566, Type: Literature]
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45
[SID103454583]
Volume of distribution was determined in rats at a single dose of 10 mg/kg i.v. and p.o. [AID236575, Type: Literature]
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46
[SID103454583]
Tmax in rat at 10 mg/kg, iv and po [AID271959, Type: Literature]
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47
[SID103454583]
Plasma half life in rat at 10 mg/kg, iv and po [AID271960, Type: Literature]
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48
[SID103454583]
Mean residence time in rat at 10 mg/kg, iv and po [AID271961, Type: Literature]
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49
[SID103454583]
Plasma clearance in rat at 10 mg/kg, iv and po [AID271962, Type: Literature]
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50
[SID103454583]
Volume of distribution in rat at 10 mg/kg, iv and po [AID271963, Type: Literature]
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