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BioAssay: AID 649259

Displacement of [3H]DPDPE from delta opioid receptor in dog brain after 90 mins by scintillation counting

3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral mu opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting changes to the lead structure which led to compounds having picomolar binding affinity, selective for the mu receptor over delta and kappa subtypes. Some subtleties of functional activity will also be described. ..more
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 Tested Compounds
 Tested Compounds
All(15)
 
 
Active(12)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(15)
 
 
Active(12)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 649259
Data Source: ChEMBL (806707)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-26

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 12
Description:
Title: SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as mu opioid ligands.

Abstract: 3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral mu opioid receptor ligands for the treatment of pruritus in dogs. In this paper, we describe the SAR of this class of opioid ligand, highlighting changes to the lead structure which led to compounds having picomolar binding affinity, selective for the mu receptor over delta and kappa subtypes. Some subtleties of functional activity will also be described.
(PMID: 22357342)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Binding
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
2Ki activity commentKi activity commentString
3Ki standard flagKi standard flagInteger
4Ki qualifierKi qualifierString
5Ki published valueKi published valueFloatnM
6Ki standard valueKi standard valueFloatnM

* Activity Concentration.

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