AID 650745 - PubChem BioAssay Summary

Plasma concentration in rat at 0.3 mg/kg after 0.75 hrs - BioAssay Summary

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

Tested Compounds

All(1)
Unspecified(1)

Tested Substances

All(1)
Unspecified(1)

Links

Related BioAssays

Depositor Specified (42)

Table of Contents

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

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Putative Target:

ChEMBL Target ID: 102352
Target Type: TISSUE
Pref Name: Plasma
Organism: Rattus norvegicus
Tax ID: 10116
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned

Categorized Comment

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ChEMBL Assay Type: ADMET

ChEMBL Assay Data Source: Scientific Literature

Result Definitions

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TID	Name	Description	Type	Unit
	Outcome	The BioAssay activity outcome	Outcome
1	Cp activity comment	Cp activity comment	String
2	Cp standard flag	Cp standard flag	Integer
3	Cp qualifier	Cp qualifier	String
4	Cp published value	Cp published value	Float	ng/ml
5	Cp standard value	Cp standard value	Float	ng/ml

Data Table (Concise)

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Data Table (Complete)

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