Target name

Q8NER1: Transient receptor potential cation channel subfamily V member 1


  Protein function

Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis (By similarity). Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel.

  Database links

Uniprot primary ID Q8NER1
PDB ID
DrugBank ID DB00168 DB00132 DB00159
BioGrid ID 113281
GuidetoPHARMACOLOGY ID 507
PharmGKB ID PA37329
KEGG ID hsa:7442
DIP ID
STRING ID 9606.ENSP00000459962
IntAct ID
DMDM 296452849
BRENDA
Reactome R-HSA-3295583
SignaLink
BioCyc
Entrez Gene (Gene ID) 7442
BindingDB Q8NER1

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.915 0.010 0.959 0.004 0.937 0.005 0.937 0.005 0.970 0.000 0.877 0.008 Download
Estate fingerprints 0.779 0.006 0.833 0.008 0.806 0.005 0.802 0.006 0.890 0.000 0.616 0.011 Download
MACCS fingerprints 0.759 0.009 0.849 0.007 0.804 0.005 0.795 0.005 0.880 0.000 0.614 0.008 Download
Daylight fingerprints 0.746 0.008 0.986 0.005 0.866 0.005 0.847 0.007 0.971 0.006 0.756 0.008 Download
ECFP2 fingerprints 0.908 0.008 0.952 0.003 0.930 0.000 0.928 0.004 0.989 0.003 0.861 0.007 Download
ECFP4 fingerprints 0.951 0.007 0.969 0.000 0.960 0.000 0.960 0.000 0.990 0.000 0.923 0.007 Download
ECFP6 fingerprints 0.919 0.006 0.981 0.000 0.950 0.005 0.949 0.003 0.990 0.000 0.903 0.007 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

The recommended browsers: Safari, Firefox, Chrome, IE(Ver.>8).
 E-mail: biomed@csu.edu.cn