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BioAssay: AID 765831

Activation of human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to U69593

(-)-Codeine 1 was converted into previously unknown 7beta-methyl-7,8-dihydrocodeine/morphine derivatives such as 13 via classical diaxial opening of alpha-epoxide 3. Several analogs exhibited dual mu/delta-agonist activity. ..more
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 Tested Compounds
 Tested Compounds
All(9)
 
 
Unspecified(9)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Unspecified(9)
 
 
 Related BioAssays
 Related BioAssays
AID: 765831
Data Source: ChEMBL (978249)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-24

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: Access to 7beta-analogs of codeine with mixed mu/delta agonist activity via 6,7-alpha-epoxide opening.

Abstract: (-)-Codeine 1 was converted into previously unknown 7beta-methyl-7,8-dihydrocodeine/morphine derivatives such as 13 via classical diaxial opening of alpha-epoxide 3. Several analogs exhibited dual mu/delta-agonist activity.
(PMID: 23880538)
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
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

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