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CHEMBL2204239 (CID 53377448) - Compound BioActivity Data
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BioActivity Outcomes:
Probe(1)
 
 
Active(3)
 
 
Inactive(18)
 
 
Unspecified(9)
 
 
Top Targets:
STKc STK33(3)
 
 
 
 
PKc like(1)
 
 
PTKc VEGFR2(1)
 
 
STKc PKA(1)
 
 
ig(1)
 
 
BioAssay Types:
Literature(28)
 
 
 
 
Confirmatory(2)
 
 
 
Summary(1)
 
 
BioActivity Types:
AC50(2)
 
 
 
IC50(2)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 31    Data Row: 31   Total Pages: 2   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID125299376]
Summary of Broad Institute MLPCN Serine Threonine Kinase 33 Inhibitor Project [AID2689, Type: summary]serine/threonine-protein kinase 33 isoform a [Homo sapiens] [gi:23943882]
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2
[SID163339240]
IC50 0.014Inhibition of N-terminal 6His-tagged full length human recombinant STK33 using myelin basic protein as substrate incubated for 15 mins before initiation of kinase reaction measured after 1 hr by ADP-glo assay [AID712545, Type: Literature]Serine/threonine-protein kinase 33 [gi:74761329]
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3
[SID125299376]
AC50_uM 7.794Counter screen for activity against Aurora B, in dose Measured in Biochemical System Using Scintillation - 2052-06_Inhibitor_Dose_DryPowder_Activity_Set3 [AID588808, Type: confirmatory]aurora kinase B isoform 1 [Homo sapiens] [gi:83776600]
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4
[SID163339240]
Solubility of the compound in PBS at pH 7.4 [AID712449, Type: Literature]
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5
[SID163339240]
IC50 10Inhibition of His-tagged recombinant catalytic fragment of PKA assessed as phosphorylation of fluorescent-labeled peptide 21substrate by caliper capillary electrophoresis [AID712541, Type: Literature]
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6
[SID163339240]
Selectivity ratio of IC50 for His-tagged recombinant catalytic fragment of PKA to IC50 for N-terminal 6His-tagged full length human recombinant STK33 [AID712544, Type: Literature]
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7
[SID163339240]
Inhibition of human FLT3 at 1 uM [AID712540, Type: Literature]Receptor-type tyrosine-protein kinase FLT3 [gi:156630887]
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8
[SID163339240]
Metabolic stability in mouse plasma at 5 uM after 5 hrs by UPLC-MS analysis [AID712445, Type: Literature]
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9
[SID163339240]
Metabolic stability in human plasma at 5 uM after 5 hrs by UPLC-MS analysis [AID712446, Type: Literature]
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10
[SID163339240]
Plasma protein binding in mouse at 5 uM after 5 hrs by equilibrium dialysis method [AID712447, Type: Literature]
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11
[SID163339240]
Plasma protein binding in human at 5 uM after 5 hrs by equilibrium dialysis method [AID712448, Type: Literature]
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12
[SID163339240]
Inhibition of N-terminal 6His-tagged full length human recombinant STK33 using myelin basic protein as substrate at 1 uM incubated for 15 mins before initiation of kinase reaction measured after 1 hr by ADP-glo assay [AID712537, Type: Literature]Serine/threonine-protein kinase 33 [gi:74761329]
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13
[SID163339240]
Inhibition of human KDR at 1 uM [AID712539, Type: Literature]Vascular endothelial growth factor receptor 2 [gi:9087218]
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14
[SID125299376]
AC50_uM Protein Kinase A Activity Assay Measured in Biochemical System Using Plate Reader - 2052-04_Inhibitor_Dose_DryPowder_Activity_Set2 [AID588629, Type: confirmatory]cAMP-dependent protein kinase catalytic subunit alpha isoform 1 [Homo sapiens] [gi:4506055]
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15
[SID163339240]
Cytotoxicity against human GDM-1 cells expressing wild type KRAS assessed as effect on cell viability up to 10 uM after 72 hrs by CellTiter-Glo luminescent assay [AID712457, Type: Literature]
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16
[SID163339240]
Cytotoxicity against human EOL-1 cells expressing wild type KRAS assessed as effect on cell viability up to 10 uM after 72 hrs by CellTiter-Glo luminescent assay [AID712458, Type: Literature]
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17
[SID163339240]
Cytotoxicity against human PL21 cells expressing wild type KRAS assessed as effect on cell viability up to 10 uM after 72 hrs by CellTiter-Glo luminescent assay [AID712459, Type: Literature]
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18
[SID163339240]
Cytotoxicity against human KARPAS620 cells expressing KRAS mutant gene assessed as effect on cell viability up to 10 uM after 72 hrs by CellTiter-Glo luminescent assay [AID712531, Type: Literature]
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19
[SID163339240]
Cytotoxicity against human RPMI8226 cells expressing KRAS mutant gene assessed as effect on cell viability up to 10 uM after 72 hrs by CellTiter-Glo luminescent assay [AID712532, Type: Literature]
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20
[SID163339240]
Cytotoxicity against human NB4 cells expressing KRAS mutant gene assessed as effect on cell viability up to 10 uM after 72 hrs by CellTiter-Glo luminescent assay [AID712533, Type: Literature]
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