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
Sequence: RecName: Full=Mu-type opioid receptor; Short=M-OR-1; Short=MOR-1
Description ..
Comment ..
Gene:OPRM1 Conserved Domain Related Protein 3D Structures
Description ..
Comment ..
Gene:OPRM1 Conserved Domain Related Protein 3D Structures
BioActive Compound: 1
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: Functional
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 100044
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 100044
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 | Kd* | Kd PubChem standard value |  | Float | μM | |
| 2 | Inhibition activity comment | Inhibition activity comment | String | |||
| 3 | Inhibition standard flag | Inhibition standard flag | | Integer | ||
| 4 | Inhibition qualifier | Inhibition qualifier | String | |||
| 5 | Inhibition published value | Inhibition published value | | Float | % | |
| 6 | Inhibition standard value | Inhibition standard value | | Float | % | |
| 7 | Kd activity comment | Kd activity comment | String | |||
| 8 | Kd standard flag | Kd standard flag | | Integer | ||
| 9 | Kd qualifier | Kd qualifier | String | |||
| 10 | Kd published value | Kd published value | | Float | nM | |
| 11 | Kd standard value | Kd standard value | | Float | nM |
* Activity Concentration.
Data Table (Concise)
Classification
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