Bookmark and Share
BioAssay: AID 649257

Antagonist activity at mu opioid receptor in guinea pig longitudinal muscle myenteric plexus assessed as inhibition of DAMGO-induced twitch tension at 1 uM after 10 mins

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
_
   
 Tested Compounds
 Tested Compounds
All(8)
 
 
Active(1)
 
 
Unspecified(7)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Active(1)
 
 
Unspecified(7)
 
 
AID: 649257
Data Source: ChEMBL (806705)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Mu-type opioid receptor; Short=M-OR-1; Short=MOR-1
Description ..   
Comment ..   

Gene:OPRM1     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
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.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Functional
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
2Inhibition activity commentInhibition activity commentString
3Inhibition standard flagInhibition standard flagInteger
4Inhibition qualifierInhibition qualifierString
5Inhibition published valueInhibition published valueFloat%
6Inhibition standard valueInhibition standard valueFloat%
7Inhibition binding domainsInhibition binding domainsString
8Kd activity commentKd activity commentString
9Kd standard flagKd standard flagInteger
10Kd qualifierKd qualifierString
11Kd published valueKd published valueFloat
12Kd standard valueKd standard valueFloatnM
13Kd binding domainsKd binding domainsString

* Activity Concentration.

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