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BioAssay: AID 621426

Metabolic stability in rat liver microsomes

Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 621426
Data Source: ChEMBL (771437)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-08-24

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BioActive Compound: 1
Description:
Title: Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.

Abstract: Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats.
(PMID: 21873051)
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 - additional comments and annotations
From BioAssay Depositor:
Assay Type: ADME
Assay Data Source: Scientific Literature
Assay Subcellular Fraction: Microsomes
Assay Tissue: Liver
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Stabilty activity commentStabilty activity commentString
2Stabilty standard flagStabilty standard flagInteger
3Stabilty qualifierStabilty qualifierString
4Stabilty published valueStabilty published valueFloat
5Stabilty standard valueStabilty standard valueFloat

Data Table (Concise)
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