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BioAssay: AID 719287

Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50,488-induced [35S]GTPgammaS binding after 60 mins by scintillation counting relative to untreated-control

N-[2-(4'-methoxy[1,1'-biphenyl]-4-yl)ethyl]-8-CAC (1) is a high affinity (K(i)=0.084 nM) ligand for the mu opioid receptor and served as the lead compound for this study. Analogues of 1 were made in hopes of identifying an SAR within a series of oxygenated (distal) phenyl derivatives. A number of new analogues were made having single-digit pM affinity for the mu receptor. The most potent was the 3',4'-methylenedioxy analogue 18 (K(i)=1.6 pM). ..more
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 Tested Compounds
 Tested Compounds
All(8)
 
 
Inactive(8)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Inactive(8)
 
 
 Related BioAssays
 Related BioAssays
AID: 719287
Data Source: ChEMBL (887030)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Kappa-type opioid receptor; Short=K-OR-1; Short=KOR-1
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx
Comment ..   

Gene:OPRK1     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.

Abstract: N-[2-(4'-methoxy[1,1'-biphenyl]-4-yl)ethyl]-8-CAC (1) is a high affinity (K(i)=0.084 nM) ligand for the mu opioid receptor and served as the lead compound for this study. Analogues of 1 were made in hopes of identifying an SAR within a series of oxygenated (distal) phenyl derivatives. A number of new analogues were made having single-digit pM affinity for the mu receptor. The most potent was the 3',4'-methylenedioxy analogue 18 (K(i)=1.6 pM).
(PMID: 23142613)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: CHO
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Imax activity commentImax activity commentString
2Imax standard flagImax standard flagInteger
3Imax qualifierImax qualifierString
4Imax published valueImax published valueFloat
5Imax standard valueImax standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View All Data
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