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
BioActive Compounds: 12
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.
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
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
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Data Source: Scientific Literature
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Ki* | Ki PubChem standard value |  | Float | μM | |
| 2 | Ki activity comment | Ki activity comment | String | |||
| 3 | Ki standard flag | Ki standard flag | | Integer | ||
| 4 | Ki qualifier | Ki qualifier | String | |||
| 5 | Ki published value | Ki published value | | Float | nM | |
| 6 | Ki standard value | Ki standard value | | Float | nM |
* Activity Concentration.
Data Table (Concise)
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