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 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)
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
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
ChEMBL Assay Type: ADMET
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Test Type: In vitro
ChEMBL Assay Tissue: Liver
ChEMBL Assay Subcellular Fraction: Microsomes
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Test Type: In vitro
ChEMBL Assay Tissue: Liver
ChEMBL Assay Subcellular Fraction: Microsomes
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | T1/2 activity comment | T1/2 activity comment | String | |||
| 2 | T1/2 standard flag | T1/2 standard flag |  | Integer | ||
| 3 | T1/2 qualifier | T1/2 qualifier | String | |||
| 4 | T1/2 published value | T1/2 published value | | Float | hr | |
| 5 | T1/2 standard value | T1/2 standard value | | Float | hr |
Data Table (Concise)
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