CHEMBL448753 (CID 24881674) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(5)
 
 
Unspecified(8)
 
 
Top Targets:
Amidase(2)
 
 
BioAssay Types:
Literature(13)
 
 
 
BioActivity Types:
IC50(2)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 13    Data Row: 13   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103611488]
IC50 0.03388Displacement of [3H]-anandamide from rat brain FAAH after 30 mins by scintillation counting [AID618766, Type: Literature]Fatty-acid amide hydrolase 1 [gi:6225312]
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2
[SID103611488]
IC50 0.034Inhibition of FAAH in rat brain membrane assessed as [3H]anandamide hydrolysis [AID404765, Type: Literature]Fatty-acid amide hydrolase 1 [gi:6225312]
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3
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant luteinizing hormone activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414565, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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4
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant luteinizing hormone activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414565, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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5
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant luteinizing hormone activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414565, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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6
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant human chorionic gonadotropin activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414566, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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7
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant human chorionic gonadotropin activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414566, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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8
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant human chorionic gonadotropin activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414566, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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9
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in Org 43553 activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414567, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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10
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in Org 43553 activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414567, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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11
[SID103611488]
 Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in Org 43553 activation potency at 10 uM by c-AMP-mediated luciferase assay [AID414567, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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12
[SID103611488]
 Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells assessed as increase in radioligand dissociation at 10 uM by scintillation spectrometry relative to control [AID414561, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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13
[SID103611488]
 Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells assessed as increase in radioligand dissociation at 10 uM by scintillation spectrometry relative to control [AID414561, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
View
14
[SID103611488]
 Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells assessed as increase in radioligand dissociation at 10 uM by scintillation spectrometry relative to control [AID414561, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
View
15
[SID103611488]
 Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells at 10 uM by scintillation spectrometry [AID414560, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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16
[SID103611488]
 Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells at 10 uM by scintillation spectrometry [AID414560, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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17
[SID103611488]
 Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells at 10 uM by scintillation spectrometry [AID414560, Type: Literature]Lutropin-choriogonadotropic hormone receptor [gi:281185513]
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18
[SID103611488]
 Hydrolytic rate constant, log k of the compound in Wistar rat plasma [AID618828, Type: Literature]
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19
[SID103611488]
 Hydrolytic rate constant, log k of the compound in Wistar rat liver S9 fraction [AID618829, Type: Literature]
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20
[SID103611488]
 Metabolic stability of the compound in Wistar rat plasma assessed as half life at 1 uM by RP-HPLC analysis [AID618764, Type: Literature]
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21
[SID103611488]
 Chemical stability of the compound in 0.01 M borate buffer assessed as half life at pH 9.0 by HPLC analysis [AID618763, Type: Literature]
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22
[SID103611488]
 Chemical stability of the compound in 0.01 M PBS assessed as compound remaining at pH 7.0 by HPLC analysis [AID618762, Type: Literature]
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23
[SID103611488]
 Metabolic stability of the compound in Wistar rat liver S9 fraction assessed as half life at 1 uM by RP-HPLC analysis [AID618765, Type: Literature]
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