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.
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 |
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 |
Positive dataset | Negative dataset |
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E-mail: biomed@csu.edu.cn