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BioAssay: AID 650614

Displacement of [125I]-DOI from recombinant human 5HT2C receptor

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(23)
 
 
Active(23)
 
 
 Tested Substances
 Tested Substances
All(23)
 
 
Active(23)
 
 
AID: 650614
Data Source: ChEMBL (808062)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=5-hydroxytryptamine receptor 2C; Short=5-HT-2C; Short=5-HT2C; Short=5-HTR2C; AltName: Full=5-hydroxytryptamine receptor 1C; Short=5-HT-1C; Short=5-HT1C; AltName: Full=Serotonin receptor 2C; Flags: Precursor
Description ..   
Protein Family: Olfactory receptor
Comment ..   

Gene:HTR2C     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 23
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
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Ki activity commentKi activity commentString
7Ki standard flagKi standard flagInteger
8Ki qualifierKi qualifierString
9Ki published valueKi published valueFloatnM
10Ki standard valueKi standard valueFloatnM
11Ki binding domainsKi binding domainsString

* Activity Concentration.

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