Target name

O35433: 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. 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. 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.

  Database links

Uniprot primary ID O35433
PDB ID 3SUI 3J9J 3J5P 3J5Q 3J5R 2NYJ 2PNN
DrugBank ID
BioGrid ID 249845
GuidetoPHARMACOLOGY ID 507
PharmGKB ID
KEGG ID rno:83810
DIP ID DIP-56949N
STRING ID 10116.ENSRNOP00000026493
IntAct ID O35433
DMDM
BRENDA
Reactome R-RNO-3295583
SignaLink
BioCyc
Entrez Gene (Gene ID) 83810
BindingDB O35433

  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 0.910 0.000 0.930 0.000 0.920 0.000 0.920 0.000 0.980 0.000 0.840 0.000 Download
Estate fingerprints 0.840 0.000 0.840 0.003 0.840 0.000 0.840 0.000 0.910 0.000 0.679 0.003 Download
MACCS fingerprints 0.726 0.005 0.868 0.000 0.797 0.005 0.780 0.000 0.902 0.004 0.598 0.004 Download
Daylight fingerprints 0.755 0.005 0.805 0.000 0.780 0.000 0.771 0.003 0.820 0.000 0.558 0.004 Download
ECFP2 fingerprints 0.927 0.005 0.953 0.000 0.940 0.000 0.940 0.000 0.980 0.000 0.878 0.004 Download
ECFP4 fingerprints 0.946 0.005 0.986 0.005 0.966 0.005 0.965 0.005 0.990 0.000 0.929 0.003 Download
ECFP6 fingerprints 0.930 0.000 0.990 0.000 0.960 0.000 0.960 0.000 0.990 0.000 0.926 0.005 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.

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