SureCN4328813 (CID 24882716) - BioAssay Data Summary for Compound
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BioActivity Outcomes:
Active(26)
 
 
Top Targets:
Orexin rec2(2)
 
 
BioAssay Types:
Literature(26)
 
 
BioActivity Types:
Ki(9)
 
 
IC50(4)
 
 
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Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 26    Data Row: 26   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103614589]
Ki 0.00059Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R expressed in CHO cells after 3 hrs by scintillation counting [AID482635, Type: Literature]Orexin receptor type 2 [gi:206729885]
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2
[SID103614589]
Ki 0.00059Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R expressed in CHO cells after 3 hrs by scintillation counting [AID482635, Type: Literature]Orexin receptor type 2 [gi:206729885]
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3
[SID103614589]
Ki 0.0006Binding affinity to OX2R [AID489200, Type: Literature]
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4
[SID103614589]
Ki 0.0006Binding affinity to OX2 receptor [AID352287, Type: Literature]
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5
[SID103614589]
Ki 0.0006Binding affinity to OX2 receptor by radioligand displacement assay [AID474967, Type: Literature]
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6
[SID103614589]
Ki 0.0012Binding affinity to OX1 receptor by radioligand displacement assay [AID474966, Type: Literature]
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7
[SID103614589]
Ki 0.0012Binding affinity to OX1R [AID489199, Type: Literature]
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8
[SID103614589]
Ki 0.0012Binding affinity to OX1 receptor [AID352286, Type: Literature]
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9
[SID103614589]
Ki 0.0012Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in CHO cells after 3 hrs by scintillation counting [AID482633, Type: Literature]Orexin receptor type 1 [gi:205804177]
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10
[SID103614589]
Ki 0.0012Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expressed in CHO cells after 20 hrs by scintillation counting [AID482634, Type: Literature]Orexin receptor type 1 [gi:205804177]
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11
[SID103614589]
Ki 0.0012Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in CHO cells after 3 hrs by scintillation counting [AID482633, Type: Literature]Orexin receptor type 1 [gi:205804177]
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12
[SID103614589]
Ki 0.0012Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expressed in CHO cells after 20 hrs by scintillation counting [AID482634, Type: Literature]Orexin receptor type 1 [gi:205804177]
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13
[SID103614589]
IC50 0.027Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay [AID482637, Type: Literature]Orexin receptor type 2 [gi:206729885]
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14
[SID103614589]
IC50 0.027Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay [AID482637, Type: Literature]Orexin receptor type 2 [gi:206729885]
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15
[SID103614589]
IC50 0.027Antagonist activity at OX2 receptor assessed as inhibition of calcium flux by FLIPR assay [AID474969, Type: Literature]
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16
[SID103614589]
IC50 0.029Antagonist activity at OX1 receptor assessed as inhibition of calcium flux by FLIPR assay [AID474968, Type: Literature]
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17
[SID103614589]
IC50 0.029Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay [AID482636, Type: Literature]Orexin receptor type 1 [gi:205804177]
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18
[SID103614589]
IC50 0.029Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium mobilization after 5 mins by FLIPR assay [AID482636, Type: Literature]Orexin receptor type 1 [gi:205804177]
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19
[SID103614589]
 Cmax in dog at 3 mg/kg, po and 0.125 mg/kg, iv [AID489205, Type: Literature]
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20
[SID103614589]
 Cmax in Sprague-Dawley rat at 10 mg/kg, po and 2 mg/kg, iv [AID489210, Type: Literature]
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21
[SID103614589]
 Cmax in dog at 3 mg/kg, po [AID482648, Type: Literature]
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22
[SID103614589]
 Antiinsomnic activity in Sprague-Dawley rat assessed as decrease in active wake duration at 10 mg/kg/day, po 30 mg/kg/day [AID482824, Type: Literature]
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23
[SID103614589]
 Antiinsomnic activity in Sprague-Dawley rat assessed as increase in rapid-eye movement at 10 mg/kg/day, po measured with 3 to 4 hrs post last dose [AID482825, Type: Literature]
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24
[SID103614589]
 Antiinsomnic activity in Sprague-Dawley rat assessed as increase in delta sleep duration at 10 mg/kg/day, po measured with 3 to 4 hrs post last dose [AID482826, Type: Literature]
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25
[SID103614589]
 Antiinsomnic activity in Sprague-Dawley rat assessed as decrease in light sleep duration at 10 mg/kg/day, po measured with 3 to 4 hrs post last dose [AID482827, Type: Literature]
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26
[SID103614589]
 Drug level in Sprague-Dawley rat plasma at 2 mg/kg, iv after 30 mins [AID474970, Type: Literature]
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27
[SID103614589]
 Drug level in Sprague-Dawley rat brain at 2 mg/kg, iv after 30 mins [AID474971, Type: Literature]
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28
[SID103614589]
 Drug level in Sprague-Dawley rat CSF at 2 mg/kg, iv after 30 mins [AID474972, Type: Literature]
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29
[SID103614589]
 Cmax in rat at 10 mg/kg, po and 2 mg/kg, iv [AID474985, Type: Literature]
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30
[SID103614589]
 Cmax in dog [AID474986, Type: Literature]
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31
[SID103614589]
 Cmax in rat at 100 mg/kg, po [AID482642, Type: Literature]
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