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BioAssay: AID 650610

Drug uptake in rat brain at 0.3 mg/kg after 0.75 hrs

A series of fused bicyclic heterocycles was identified as potent and selective 5-HT(2A) receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 650610
Data Source: ChEMBL (808058)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Tested Compound:
Description:
Title: Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.

Abstract: A series of fused bicyclic heterocycles was identified as potent and selective 5-HT(2A) receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation.
(PMID: 22325948)
Comment
Putative Target:
ChEMBL Target ID: 102317
Target Type: TISSUE
Pref Name: Brain
Organism: Rattus norvegicus
Tax ID: 10116
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: ADME
Assay Data Source: Scientific Literature
BAO: Assay Format: organism-based format
Assay Tissue: Brain
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Drug uptake activity commentDrug uptake activity commentString
2Drug uptake standard flagDrug uptake standard flagInteger
3Drug uptake qualifierDrug uptake qualifierString
4Drug uptake published valueDrug uptake published valueFloatng/ml
5Drug uptake standard valueDrug uptake standard valueFloatng/ml

Data Table (Concise)
Data Table ( Complete ):     View All Data
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