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BioAssay: AID 621428

Metabolic stability in human 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: 621428
Data Source: ChEMBL (771439)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
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: 102164
Target Type: SUBCELLULAR
Pref Name: Liver microsomes
Organism: Homo sapiens
Tax ID: 9606
Confidence: Target assigned is subcellular fraction
Relationship Type: Subcellular target assigned
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: subcellular format

Assay Tissue: Liver

Assay Subcellular Fraction: Microsomes

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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