Target name

P41145: Kappa-type opioid receptor


  Protein 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

Uniprot primary ID P41145
GRCP SARfari Variant Name hOPRK1_173
PDB ID 4DJH 2IQN 2A0D
DrugBank ID DB06148 DB00899 DB00652 DB00497 DB00327 DB00321 DB00813 DB00825 DB00854 DB06204 DB00836 DB00370 DB00704 DB00611 DB00708 DB00647 DB00318 DB00921 DB00295 DB00396 DB06274 DB01183 DB00844 DB00514 DB01209 DB01221 DB00454 DB06738 DB06800 DB00193 DB01452
BioGrid ID 111031
GuidetoPHARMACOLOGY ID 318
PharmGKB ID PA31943
KEGG ID hsa:4986
Entrez Gene (Gene ID) 4986
BindingDB P41145

  Model Performance Metrics

Fingerprint type Sensitivity Specificity Accuracy F1-score AUC Matthews_corrcoef Download model
FP2 fingerprints 0.76 0.71 0.74 0.74 0.8 0.47 Download
FP4 fingerprints 0.800 0.710 0.750 0.760 0.820 0.510 Download
MACCS fingerprints 0.790 0.650 0.720 0.740 0.780 0.450 Download
Daylight fingerprints 0.600 0.770 0.680 0.650 0.730 0.370 Download
ECFP2 fingerprints 0.800 0.840 0.820 0.820 0.880 0.650 Download
ECFP4 fingerprints 0.800 0.890 0.840 0.830 0.890 0.690 Download
ECFP6 fingerprints 0.760 0.900 0.830 0.820 0.890 0.670 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2015 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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