TargetNet


P41145

Kappa-type opioid receptor


Function

G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions.


Database Links

Database Links
UniProt P41145
PDB 2A0D, 2IQN, 4DJH
BioGrid 111031
BindingDB P41145
DrugBank DB00921, DB00611, DB00907, DB00318, DB01209, DB00956, DB00327, DB00454, DB00370, DB00295, DB00844, DB00704, DB00497, DB00652, DB00647, DB00193
Guide to PHARMACOLOGY 318
PharmGKB PA31943
KEGG hsa:4986
BioCyc Not available
Entrez Gene (GeneID) 4986

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.9528 0.0011
Accuracy 0.9067 0.002
Sensitivity 0.89 0.0021
Specificity 0.9227 0.0031
BEDROC 0.9812 0.0017
MCC Threshold 0.496 N/A
MCC 0.8119 N/A
F-score Threshold 0.468 N/A
F-score 0.9027 N/A

Downloads

R Model Object

Random Forest model object (.RData)

Download RData

Positive Set

SMILES string + affinity value (.tsv)

Download TSV


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Page generated on: 2014-04-29 14:39:38