Bookmark and Share
BioAssay: AID 648313

Inhibition of CYP3A4 in human liver microsomes

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
_
   
 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 648313
Data Source: ChEMBL (805761)
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 ):           All
Target
Sequence: RecName: Full=Cytochrome P450 3A4; AltName: Full=1,8-cineole 2-exo-monooxygenase; AltName: Full=Albendazole monooxygenase; AltName: Full=Albendazole sulfoxidase; AltName: Full=CYPIIIA3; AltName: Full=CYPIIIA4; AltName: Full=Cytochrome P450 3A3; AltName: Full=Cytochrome P450 HLp; AltName: Full=Cytochrome P450 NF-25; AltName: Full=Cytochrome P450-PCN1; AltName: Full=Nifedipine oxidase; AltName: Full=Quinine 3-monooxygenase; AltName: Full=Taurochenodeoxycholate 6-alpha-hydroxylase
Description ..   
Protein Family: Cytochrome P450
Comment ..   

Gene:CYP3A4     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
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)
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: subcellular format

Assay Tissue: Liver

Assay Subcellular Fraction: Microsomes

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 valueFloatμM
6IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
PageFrom: