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CHEMBL1921850 (CID 56849550) - Compound BioActivity Data
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BioActivity Outcomes:
Active(5)
 
 
Inactive(3)
 
 
Unspecified(7)
 
 
Top Targets:
7TM GPCR Srx(9)
 
 
 
 
BioAssay Types:
Literature(15)
 
 
 
 
BioActivity Types:
Ki(3)
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 15    Data Row: 15   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID136931600]
Ki 0.00105Displacement of [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting [AID631359, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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2
[SID136931600]
Ki 0.0431Displacement of [3H]diprenorphine from human opioid mu receptor expressed in CHO cells after 120 mins by scintillation counting [AID631360, Type: Literature]Mu-type opioid receptor [gi:2851402]
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3
[SID136931600]
Antagonist activity at human opioid mu receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTP-gamma-S binding after 4 hrs by scintillation counting [AID631365, Type: Literature]Mu-type opioid receptor [gi:2851402]
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4
[SID136931600]
Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U69593-induced [35S]GTP-gamma-S binding after 4 hrs by scintillation counting [AID631364, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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5
[SID136931600]
Antagonist activity at human opioid delta receptor expressed in HEK293 cells assessed as inhibition of DPDPE-induced [35S]GTP-gamma-S binding after 4 hrs by scintillation counting [AID631347, Type: Literature]Delta-type opioid receptor [gi:311033488]
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6
[SID136931600]
Ki 0.5Displacement of [3H]diprenorphine from human opioid delta receptor expressed in HEK293 cells after 120 mins by scintillation counting [AID631361, Type: Literature]Delta-type opioid receptor [gi:311033488]
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7
[SID136931600]
Selectivity ratio of Kb for human opioid mu receptor expressed in CHO cells to Kb for human opioid kappa receptor expressed in CHO cells [AID631348, Type: Literature]
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8
[SID136931600]
Selectivity ratio of Ki for human opioid mu receptor expressed in CHO cells to Ki for human opioid kappa receptor expressed in CHO cells [AID631362, Type: Literature]
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9
[SID136931600]
Selectivity ratio of Ki for human opioid delta receptor expressed in HEK293 cells to Ki for human opioid kappa receptor expressed in CHO cells [AID631363, Type: Literature]
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10
[SID136931600]
Selectivity ratio of Kb for human opioid delta receptor expressed in HEK293 cells to Kb for human opioid kappa receptor expressed in CHO cells [AID631391, Type: Literature]
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11
[SID136931600]
Drug uptake in rat striatum at 1 ug/kg, iv measured after 40 mins by LC/MS-MS analysis [AID631400, Type: Literature]
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12
[SID136931600]
Ratio of drug uptake in striatum to cerebellum in rat at 1 ug/kg, iv measured after 40 mins by LC/MS/MS analysis [AID631404, Type: Literature]
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13
[SID136931600]
Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding at 10 uM [AID631392, Type: Literature]Kappa-type opioid receptor [gi:116242691]
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14
[SID136931600]
Agonist activity at human opioid mu receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding at 10 uM [AID631393, Type: Literature]Mu-type opioid receptor [gi:2851402]
View
15
[SID136931600]
Agonist activity at human opioid delta receptor expressed in HEK293 cells assessed as stimulation of [35S]-GTPgammaS binding at 10 uM [AID631394, Type: Literature]Delta-type opioid receptor [gi:311033488]
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