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BioAssay: AID 646687

Metabolic stability in human liver microsomes

An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. gamma-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues. ..more
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Inconclusive(1)
 
 
Unspecified(11)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Inconclusive(1)
 
 
Unspecified(11)
 
 
 Related BioAssays
 Related BioAssays
AID: 646687
Data Source: ChEMBL (804135)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-11-17

Data Table ( Complete ):           All
Tested Compounds:
Description:
Title: gamma-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.

Abstract: An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. gamma-Carbolines are a novel class of potent mixed CB1/CB2 agonists characterized by attractive physicochemical properties including high aqueous solubility. Optimization of the series has led to the discovery of 29, which has oral activity in a rat inflammatory pain model and limited brain exposure at analgesic doses, consistent with a lower risk of CNS-mediated tolerability issues.
(PMID: 22284817)
Comment
Putative Target:

ChEMBL Target ID: 102164
Target Type: SUBCELLULAR
Pref Name: Liver microsomes
Organism: Homo sapiens
Tax ID: 9606
Confidence: Target assigned is subcellular fraction
Relationship Type: Subcellular target assigned
Categorized Comment
ChEMBL Assay Type: ADMET

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Assay Tissue: Liver

ChEMBL Assay Subcellular Fraction: Microsomes

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Stabilty activity commentStabilty activity commentString
2Stabilty standard flagStabilty standard flagInteger
3Stabilty qualifierStabilty qualifierString
4Stabilty published valueStabilty published valueFloatmicroL/min/mg
5Stabilty standard valueStabilty standard valueFloatmicroL/min/mg

Data Table (Concise)
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