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CHEMBL2037200 (CID 44545852) - Compound BioActivity Data
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BioActivity Outcomes:
Active(7)
 
 
Unspecified(19)
 
 
Top Targets:
PKc(5)
 
 
 
ig(1)
 
 
BioActivity Types:
IC50(6)
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 26    Data Row: 26   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID160673717]
IC50 0.005Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate by radiometric assay [AID663798, Type: other]Serine/threonine-protein kinase pim-1 [gi:83305339]
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2
[SID160673717]
Ki 0.005Reversible inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate [AID663811, Type: other]Serine/threonine-protein kinase pim-1 [gi:83305339]
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3
[SID160673717]
IC50 0.016Inhibition of Pim3 using RSRHSSYPAGT as substrate by radiometric assay [AID663806, Type: other]
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4
[SID160673717]
IC50 0.025Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay [AID663799, Type: other]Serine/threonine-protein kinase pim-2 [gi:20139243]
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5
[SID160673717]
IC50 0.134Inhibition of Flt3 using EAIYAAPFAKKK as substrate by radiometric assay [AID663805, Type: other]
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6
[SID160673717]
IC50 0.452Cytotoxicity against human PC3 cells assessed as viability after 96 hrs [AID663816, Type: other]
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7
[SID160673717]
Drug metabolism in mouse assessed as formation of 3-((5-(3-(1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)-5-chloroindolin-2-one [AID663824, Type: other]
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8
[SID160673717]
IC50 10Inhibition of Flt3 phosphorylation at Y591 in human MV411 cells after 2 hrs by Western blot analysis [AID663815, Type: other]Receptor-type tyrosine-protein kinase FLT3 [gi:156630887]
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9
[SID160673717]
Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate at 0.5 uM by radiometric assay [AID663807, Type: other]Serine/threonine-protein kinase pim-1 [gi:83305339]
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10
[SID160673717]
Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate at 0.5 uM by radiometric assay [AID663808, Type: other]Serine/threonine-protein kinase pim-2 [gi:20139243]
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11
[SID160673717]
Antitumor activity against human MV411 cells xenografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po administered qd for 21 days relative to vehicle treated control [AID663817, Type: other]
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12
[SID160673717]
Antitumor activity against human MV411 cells xenografted in nude mouse assessed as tumor growth inhibition at 100 mg/kg, po administered qd for 21 days relative to vehicle treated control [AID663818, Type: other]
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13
[SID160673717]
Antitumor activity against human MV411 cells xenografted in po dosed nude mouse assessed as tumor growth inhibition administered qd for 21 days [AID663819, Type: other]
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14
[SID160673717]
Antitumor activity against human PC3 cells xenografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, ip administered qd 5 days a week for 33 days relative to vehicle treated control [AID663820, Type: other]
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15
[SID160673717]
Toxicity in human MV411 cells xenografted nude mouse assessed as mortality at 50 to 100 mg/kg, po qd for 21 days [AID663822, Type: other]
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16
[SID160673717]
Toxicity in human PC3 cells xenografted nude mouse assessed as mortality at 50 to 100 mg/kg, po qd for 21 days [AID663823, Type: other]
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17
[SID160673717]
Inhibition of Pim3 using RSRHSSYPAGT as substrate at 0.5 uM by radiometric assay [AID663809, Type: other]
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18
[SID160673717]
Inhibition of Flt3 using EAIYAAPFAKKK as substrate at 0.5 uM by radiometric assay [AID663810, Type: other]
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19
[SID160673717]
Inhibition of Pim-mediated Bad phosphorylation at Ser112 in human MV411 cells after 2 hrs by Western blot analysis [AID663812, Type: other]
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20
[SID160673717]
Inhibition of Pim-mediated 4E-BP1 phosphorylation at Ser65 in human MV411 cells after 2 hrs by Western blot analysis [AID663813, Type: other]
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21
[SID160673717]
Inhibition of Pim-mediated 4E-BP1 phosphorylation at T-36/47 in human MV411 cells after 2 hrs by Western blot analysis [AID663814, Type: other]
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22
[SID160673717]
Clearance in iv dosed mouse [AID663800, Type: other]
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23
[SID160673717]
Volume of distribution in iv dosed mouse [AID663801, Type: other]
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24
[SID160673717]
Half life in iv dosed mouse [AID663802, Type: other]
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25
[SID160673717]
AUC (0 to 24 hrs) in po dosed mouse [AID663803, Type: other]
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26
[SID160673717]
Oral bioavailability in mouse [AID663804, Type: other]
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