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BioAssay: AID 650747

Half life in rat liver microsomes

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: 650747
Data Source: ChEMBL (808195)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-26

Data Table ( Complete ):           All
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: 102178
Target Type: SUBCELLULAR
Pref Name: Liver microsomes
Organism: Rattus norvegicus
Tax ID: 10116
Confidence: Target assigned is subcellular fraction
Relationship Type: Subcellular target assigned
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: subcellular format

Assay Tissue: Liver

Assay Subcellular Fraction: Microsomes

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1T1/2 activity commentT1/2 activity commentString
2T1/2 standard flagT1/2 standard flagInteger
3T1/2 qualifierT1/2 qualifierString
4T1/2 published valueT1/2 published valueFloatmin
5T1/2 standard valueT1/2 standard valueFloathr

Data Table (Concise)
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