3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral ## 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 ## receptor over ## and ## subtypes. Some subtleties of functional activity will also be described. ..more
Target
BioActive Compounds: 4
Description:
Title: SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as ## opioid ligands.
Abstract: 3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral ## 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 ## receptor over ## and ## subtypes. Some subtleties of functional activity will also be described.
(PMID: 22357342)
Abstract: 3-Azabicyclo[3.1.0]hexane compounds were designed as novel achiral ## 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 ## receptor over ## and ## 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
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 129
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 129
ChEMBL target type: Target is a single protein chain
Result Definitions
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| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Ki* | Ki PubChem standard value |  | Float | μM | |
| 2 | BEI | Binding Efficiency Index(nM) | | Float | ||
| 3 | SEI | Surface Efficiency Index(nM) | | Float | ||
| 4 | Ki activity comment | Ki activity comment | String | |||
| 5 | Ki standard flag | Ki standard flag | | Integer | ||
| 6 | Ki qualifier | Ki qualifier | String | |||
| 7 | Ki published value | Ki published value | | Float | nM | |
| 8 | Ki standard value | Ki standard value | | Float | nM | |
| 9 | Ki binding domains | Ki binding domains | String |
* Activity Concentration.
Data Table (Concise)
Classification
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