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BioAssay: AID 397455

Critical micelle concentration by drop-shape analysis

This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTPgammaS to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTPgammaS and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results. ..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
AID: 397455
Data Source: ChEMBL (545484)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-16

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: [35S]GTP gamma S binding studies of amphiphilic drugs-activated Gi proteins: a caveat.

Abstract: This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTPgammaS to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTPgammaS and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results.
(PMID: 19289280)
Comment
Putative Target:

ChEMBL Target ID: 22229
Target Type: NO TARGET
Pref Name: No relevant target
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Physicochemical

Assay Data Source: Scientific Literature

BAO: Assay Format: small-molecule physicochemical format

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1CMC activity commentCMC activity commentString
2CMC standard flagCMC standard flagInteger
3CMC qualifierCMC qualifierString
4CMC published valueCMC published valueFloat10'-4M
5CMC standard valueCMC standard valueFloatμM

Data Table (Concise)
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