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BioAssay: AID 648325

Metabolic stability in human liver microsomes assessed as CYP3A4-mediated glutathione adduct formation by glutathione conjugation assay

Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy in the rat chronic constriction injury (CCI)-induced model of neuropathic pain is described. ..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: 648325
Data Source: ChEMBL (805773)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

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BioActive Compound: 1
Description:
Title: Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.

Abstract: Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy in the rat chronic constriction injury (CCI)-induced model of neuropathic pain is described.
(PMID: 22330635)
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

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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