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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL237
Target Type SINGLE PROTEIN
Preferred Name Kappa opioid receptor
Synonyms K-OR-1 | KOR-1 | Kappa-type opioid receptor | OPRK | OPRK1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > peptide receptor (family a gpcr) > short peptide receptor (family a gpcr) > opioid receptor

Target Components

Component Description Relationship Accession
Kappa-type opioid receptor SINGLE PROTEIN P41145

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2095151 Opioid receptors; delta & kappa SELECTIVITY GROUP
CHEMBL2095156 Opioid receptors; mu & kappa SELECTIVITY GROUP
CHEMBL2095181 Opioid receptors; mu/kappa/delta PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL299400 BUTORPHANOL TARTRATE Kappa opioid receptor partial agonist 4 DailyMed
CHEMBL511142 BUPRENORPHINE Kappa opioid receptor agonist 4 DailyMed PubMed
CHEMBL1685 DEZOCINE Kappa opioid receptor antagonist 4 ISBN PubMed
CHEMBL1200543 ANILERIDINE PHOSPHATE Kappa opioid receptor agonist 4 Expert PubMed
CHEMBL1201047 ANILERIDINE HYDROCHLORIDE Kappa opioid receptor agonist 4 Expert PubMed
CHEMBL2062276 LEVALLORPHAN TARTRATE Kappa opioid receptor partial agonist 4 PubMed
CHEMBL2368861 BUPRENORPHINE HYDROCHLORIDE Kappa opioid receptor agonist 4 DailyMed PubMed
CHEMBL490665 NALFURAFINE HYDROCHLORIDE Kappa opioid receptor agonist 3 PubMed PubMed
CHEMBL3989680 AXOMADOL Kappa opioid receptor agonist 2

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000082556
Ensembl ENSG00000082556
GO Cellular Component GO:0005634 (nucleus)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030425 (dendrite)
GO:0043005 (neuron projection)
GO:0043025 (neuronal cell body)
GO:0043204 (perikaryon)
GO:0043679 (axon terminus)
GO:0045202 (synapse)
GO Molecular Function GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004985 (opioid receptor activity)
GO:0005515 (protein binding)
GO:0038048 (dynorphin receptor activity)
GO:0042923 (neuropeptide binding)
GO Biological Process GO:0006955 (immune response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007193 (adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway)
GO:0007200 (phospholipase C-activating G-protein coupled receptor signaling pathway)
GO:0007218 (neuropeptide signaling pathway)
GO:0007268 (chemical synaptic transmission)
GO:0007600 (sensory perception)
GO:0007610 (behavior)
GO:0007626 (locomotory behavior)
GO:0009314 (response to radiation)
GO:0019233 (sensory perception of pain)
GO:0031635 (adenylate cyclase-inhibiting opioid receptor signaling pathway)
GO:0032868 (response to insulin)
GO:0033603 (positive regulation of dopamine secretion)
GO:0033685 (negative regulation of luteinizing hormone secretion)
GO:0038003 (opioid receptor signaling pathway)
GO:0040017 (positive regulation of locomotion)
GO:0042220 (response to cocaine)
GO:0042711 (maternal behavior)
GO:0042755 (eating behavior)
GO:0043278 (response to morphine)
GO:0043627 (response to estrogen)
GO:0044849 (estrous cycle)
GO:0045471 (response to ethanol)
GO:0046877 (regulation of saliva secretion)
GO:0048148 (behavioral response to cocaine)
GO:0050951 (sensory perception of temperature stimulus)
GO:0051607 (defense response to virus)
GO:0051930 (regulation of sensory perception of pain)
GO:0071222 (cellular response to lipopolysaccharide)
GO:1900745 (positive regulation of p38MAPK cascade)
GO:1901381 (positive regulation of potassium ion transmembrane transport)
GO:1903937 (response to acrylamide)
GO:1904000 (positive regulation of eating behavior)
GO:1990708 (conditioned place preference)
Wikipedia Kappa_Opioid_receptor

Target Cross References - Protein

canSAR P41145
Human Protein Atlas ENSG00000082556
IntAct P41145
Guide to Pharmacology 318
Open Targets ENSG00000082556
PharmGKB PA31943
Pharos P41145 (Tclin)
Reactome R-HSA-375276 (Peptide ligand-binding receptors.)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt E5RHC9 P41145 Q499G4

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000452 (Kappa_opi_rcpt.)
IPR001418 (Opioid_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)

Target Cross References - Structure

PDBe 4DJH 6B73
CREDO 4DJH 6B73
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