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BioAssay: AID 648324

Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium flux by FLIPR 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(16)
 
 
Active(16)
 
 
 Tested Substances
 Tested Substances
All(16)
 
 
Active(16)
 
 
AID: 648324
Data Source: ChEMBL (805772)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
Target
Sequence: Transient receptor potential M8 protein
Description ..   
Comment ..   

     More BioActivity Data..
BioActive Compounds: 16
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
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Functional

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: HEK293

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatnM
6IC50 standard valueIC50 standard valueFloatnM
7IC50 binding domainsIC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
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