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BioAssay: AID 765840

Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay

(-)-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)
 
 
Active(7)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Active(7)
 
 
Unspecified(2)
 
 
AID: 765840
Data Source: ChEMBL (978258)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Kappa-type opioid receptor; Short=K-OR-1; Short=KOR-1
Description ..   
Protein Family: Olfactory receptor
Comment ..   

Gene:OPRK1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 7
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)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
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
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6EC50 activity commentEC50 activity commentString
7EC50 standard flagEC50 standard flagInteger
8EC50 qualifierEC50 qualifierString
9EC50 published valueEC50 published valueFloatμM
10EC50 standard valueEC50 standard valueFloatnM
11EC50 data validityEC50 data validityString

* Activity Concentration.

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