General Information of the Protein
Protein ID
PT01460
Protein Name
Kappa-type opioid receptor
Gene Name
OPRK1
Secondarily
Gene Name
Ror-d
Sequence
MESPIQIFRGEPGPTCAPSACLLPNSSSWFPNWAESDSNGSVGSEDQQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSAVYLMNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLASSVGISAIVLGGTKVREDVDVIECSLQFPDDEYSWWDLFMKICVFVFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITKLVLVVVAVFIICWTPIHIFILVEALGSTSHSTAVLSSYYFCIALGYTNSSLNPVLYAFLDENFKRCFRDFCFPIKMRMERQSTNRVRNTVQDPASMRDVGGMNKPV
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Opioid receptor
Function
G-protein coupled opioid receptor that functions as a receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as a 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.
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Uniprot ID
P34975
Ensembl ID
ENSG00000082556
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000051 , BHK-21
Compound ID Compound Name Compound Formula
CP0038839
(4R,4aS,7aR,12bS)-3-allyl-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride
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C19H21NO4
 1
1
Kd = 4.5 nM
   TI
   LI
   LO
   TS
CP0402338
8-Cycloundecyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C24H37N3O
 1
1
Ki = 0.82 nM
   TI
   LI
   LO
   TS
CP0422910
8-Cyclodecyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C23H35N3O
 1
1
Ki = 2.1 nM
   TI
   LI
   LO
   TS
CP0431654
8-Cyclododecyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C25H39N3O
 1
1
Ki = 2.9 nM
   TI
   LI
   LO
   TS
CP0405159
8-Cyclononyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C22H33N3O
 1
1
Ki = 3.9 nM
   TI
   LI
   LO
   TS
CP0441527
8-Cyclooctyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C21H31N3O
 1
1
Ki = 9.1 nM
   TI
   LI
   LO
   TS
CP0422928
8-Cycloheptyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C20H29N3O
 1
1
Ki = 12 nM
   TI
   LI
   LO
   TS
CP0038465
8-(R)-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C25H25N3O
 1
1
Ki = 20 nM
   TI
   LI
   LO
   TS
CP0437276
8-(4-Isopropyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C22H33N3O
 1
1
Ki = 26 nM
   TI
   LI
   LO
   TS
CP0402390
8-Bicyclohexyl-4-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C25H37N3O
 1
1
Ki = 29 nM
   TI
   LI
   LO
   TS
CP0460264
8-(4-Isopropyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C22H33N3O
 1
1
Ki = 31 nM
   TI
   LI
   LO
   TS
CP0414949
8-(4-tert-Butyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C23H35N3O
 1
1
Ki = 38 nM
   TI
   LI
   LO
   TS
CP0379320
8-(4-Methyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C20H29N3O
 1
1
Ki = 57 nM
   TI
   LI
   LO
   TS
CP0405179
1-Phenyl-8-(4-propyl-cyclohexyl)-1,3,8-triaza-spiro[4.5]decan-4-one
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C22H33N3O
 1
1
Ki = 57 nM
   TI
   LI
   LO
   TS
CP0402183
8-Cyclohexyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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C19H27N3O
 1
1
Ki = 100 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0038839
(4R,4aS,7aR,12bS)-3-allyl-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one;hydrochloride
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C19H21NO4
 1
1 Kd = 1 nM
CP0054764
2-[(1S,2S,13R,21R)-22-(cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15,17,19(25)-heptaen-7-yl]guanidine
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C27H29N5O3
 3
1 Ki = 0.06 nM
2 Ki = 0.14 nM
3 Ki = 12.9 nM
CP0182209
5'-[N-(N'-Cyano)guanidinyl]-17-cyclopropylmethyl-6,7-didehydro-4,5alpha-epoxy-3,14-dihydroxyindolo[2',3':6,7]morphinan
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C28H28N6O3
 2
1 Ki = 0.29 nM
2 Ki = 2.48 nM
CP0041449
C18130
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C40H43N3O6
 2
1 Ki = 0.77 nM
2 Ki = 12.5 nM
CP0101779
2-[(1S,2S,13R,21R)-22-(cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15,17,19(25)-heptaen-8-yl]guanidine
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C27H29N5O3
 1
1 Ki = 1.15 nM
CP0677668
7`-guanidino-17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,14-hydroxyindolo-[2`,3`:6,7]morphinian
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C27H29N5O3
 1
1 Ki = 69.1 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02264 Kappa-type opioid receptor Mus musculus, Mouse