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BioAssay: AID 735222

Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding relative to U69593

Dual-acting kappa opioid receptor (KOR) agonist and mu opioid receptor (MOR) partial agonist ligands have been put forward as potential treatment agents for cocaine and other psychostimulant abuse. Members of the orvinol series of ligands are known for their high binding affinity to both KOR and MOR, but efficacy at the individual receptors has not been thoroughly evaluated. In this study, it is more ..
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 Tested Compounds
 Tested Compounds
All(40)
 
 
Unspecified(40)
 
 
 Tested Substances
 Tested Substances
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Unspecified(40)
 
 
 Related BioAssays
 Related BioAssays
AID: 735222
Data Source: ChEMBL (947790)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-05-27

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: Orvinols with mixed kappa/mu opioid receptor agonist activity.

Abstract: Dual-acting kappa opioid receptor (KOR) agonist and mu opioid receptor (MOR) partial agonist ligands have been put forward as potential treatment agents for cocaine and other psychostimulant abuse. Members of the orvinol series of ligands are known for their high binding affinity to both KOR and MOR, but efficacy at the individual receptors has not been thoroughly evaluated. In this study, it is shown that a predictive model for efficacy at KOR can be derived, with efficacy being controlled by the length of the group attached to C20 and by the introduction of branching into the side chain. In vivo evaluation of two ligands with the desired in vitro profile confirms both display KOR, and to a lesser extent MOR, activity in an analgesic assay suggesting that, in this series, in vitro measures of efficacy using the [(35)S]GTPgammaS assay are predictive of the in vivo profile.
(PMID: 23438330)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: CHO

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

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