Inhibition of human thioredoxin signalling assessed as inhibition of insulin reduction at 10 uM - BioAssay Summary
The synthesis and in vitro antitumour evaluation of a new series of fluorinated benzothiazole-substituted 4-hydroxycyclohexa-2,5-dienones ('quinols') is described. The new compounds were found to be of comparable activity compared to the non-fluorinated precursor PMX 464, in terms of antiproliferative activity in sensitive human cancer cell lines (nanomolar GI(50) values) and inhibitory activity against the thioredoxin signalling system. ..more
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 271195
Data Source: ChEMBL (402467)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-05-05

Data Table (Complete):           All
Targets
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Sequence: RecName: Full=Thioredoxin reductase 1, cytoplasmic; Short=TR; AltName: Full=Gene associated with retinoic and interferon-induced mortality 12 protein; Short=GRIM-12; Short=Gene associated with retinoic and IFN-induced mortality 12 protein; AltName: Full=KM-102-derived reductase-like factor; AltName: Full=Thioredoxin reductase TR1
Description ..   
Protein Family: Pyridine nucleotide-disulphide oxidoreductase, dimerisation domain
Comment ..   

Gene:TXNRD1     Related Protein 3D Structures


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Tested Compounds:
Description:
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Title: Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols').

Abstract: The synthesis and in vitro antitumour evaluation of a new series of fluorinated benzothiazole-substituted 4-hydroxycyclohexa-2,5-dienones ('quinols') is described. The new compounds were found to be of comparable activity compared to the non-fluorinated precursor PMX 464, in terms of antiproliferative activity in sensitive human cancer cell lines (nanomolar GI(50) values) and inhibitory activity against the thioredoxin signalling system.
(PMID: 16908135)
Categorized Comment
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ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 104858

ChEMBL target type: Target is a group of closely related proteins

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
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Classification
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