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CHEMBL1923642 (CID 11526745) - Compound BioActivity Data
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BioActivity Outcomes:
Active(6)
 
 
Unspecified(18)
 
 
Top Targets:
p450(5)
 
 
 
Motilin assoc(2)
 
 
BioAssay Types:
Literature(24)
 
 
 
BioActivity Types:
IC50(5)
 
 
 
Ki(1)
 
 
EC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 24    Data Row: 24   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID136944240]
Ki 0.0026Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay [AID632805, Type: Literature]Appetite-regulating hormone [gi:17865471]
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2
[SID136944240]
EC50 0.027Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay [AID632806, Type: Literature]Appetite-regulating hormone [gi:17865471]
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3
[SID136944240]
IC50 1.2Inhibition of human CYP3A4 [AID632818, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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4
[SID136944240]
IC50 31Inhibition of human CYP2D6 [AID632819, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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5
[SID136944240]
Cmax in cynomolgus monkey at 8 mg/kg, po [AID632825, Type: Literature]
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6
[SID136944240]
Cmax in Sprague-Dawley rat at 8 mg/kg, po [AID632808, Type: Literature]
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7
[SID136944240]
IC50 100Inhibition of human CYP2C19 [AID632821, Type: Literature]Cytochrome P450 2C19 [gi:60416369]
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8
[SID136944240]
IC50 100Inhibition of human CYP1A2 [AID632822, Type: Literature]Cytochrome P450 1A2 [gi:117144]
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9
[SID136944240]
IC50 100Inhibition of human CYP2C9 [AID632820, Type: Literature]Cytochrome P450 2C9 [gi:6686268]
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10
[SID136944240]
AUC (0 to infinity) in cynomolgus monkey at 8 mg/kg, po [AID632826, Type: Literature]
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11
[SID136944240]
Elimination half life in cynomolgus monkey at 2 mg/kg, iv [AID632981, Type: Literature]
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12
[SID136944240]
Volume of distribution at steady state in cynomolgus monkey at 2 mg/kg, iv [AID632982, Type: Literature]
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13
[SID136944240]
Clearance in cynomolgus monkey at 2 mg/kg, iv [AID632983, Type: Literature]
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14
[SID136944240]
Oral bioavailability in cynomolgus monkey at 8 mg/kg [AID632984, Type: Literature]
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15
[SID136944240]
Induction of gasrtic emptying in overnight-fasted iv dosed Wistar rat measured after 15 mins by calorimetric analysis [AID632989, Type: Literature]
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16
[SID136944240]
AUC (0 to infinity) in Sprague-Dawley rat at 8 mg/kg, po [AID632809, Type: Literature]
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17
[SID136944240]
Elimination half life in Sprague-Dawley rat at 2 m/kg, iv [AID632810, Type: Literature]
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18
[SID136944240]
Volume of distribution at steady state in Sprague-Dawley rat at 2 m/kg, iv [AID632811, Type: Literature]
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19
[SID136944240]
Clearance in Sprague-Dawley rat at 2 m/kg, iv [AID632812, Type: Literature]
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20
[SID136944240]
Oral bioavailability in Sprague-Dawley rat at 2 mg/kg [AID632813, Type: Literature]
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21
[SID136944240]
Permeability across mucosal to serosal side in human Caco2 cells [AID632814, Type: Literature]
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22
[SID136944240]
Permeability across serosal to mucosal side human Caco2 cells [AID632815, Type: Literature]
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23
[SID136944240]
Drug metabolism in rat liver microsomes after 15 mins [AID632816, Type: Literature]
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24
[SID136944240]
Half life in human liver microsomes [AID632817, Type: Literature]
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