General Information of the Protein
Protein ID
PT01526
Protein Name
Delta-type opioid receptor
Secondarily
Protein Name
Opioid receptor A
Gene Name
OPRD1
Secondarily
Gene Name
Ror-a
Sequence
MEPVPSARAELQFSLLANVSDTFPSAFPSASANASGSPGARSASSLALAIAITALYSAVCAVGLLGNVLVMFGIVRYTKLKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTQPRDGAVVCTLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDINRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRAPCGGQEPGSLRRPRQATARERVTACTPSDGPGGGAAA
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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 receptor that functions as a receptor for endogenous enkephalins and for a subset of other opioids. 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 and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine.
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Uniprot ID
P33533
Ensembl ID
ENSG00000116329
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: CL000047 , 108CC15
Compound ID Compound Name Compound Formula
CP0383819
(S,3S,3'S)-N,N'-(ethane-1,2-diyl)bis(2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide)
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C44H52N6O6
 1
1
Kd = 0.912 nM
   TI
   LI
   LO
   TS
CP0390966
(S,3S,3'S)-N,N'-(hex-3-ene-1,6-diyl)bis(2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide)
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C48H58N6O6
 1
1
Kd = 1.148 nM
   TI
   LI
   LO
   TS
CP0390493
(S,S,3S,3'S,3''S)-N,N',N''-(2,2',2''-nitrilotris(ethane-2,1-diyl))tris(2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide)
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C69H84N10O9
 1
1
Kd = 2.291 nM
   TI
   LI
   LO
   TS
CP0087279
(S)-2-((S)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
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C21H24N2O4
 1
1
Kd = 3.311 nM
   TI
   LI
   LO
   TS
CP0400425
(2S,2'S)-N,N'-((4S,4'S)-2,2'-(2,2'-(ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(3-oxo-2,3,4,5-tetrahydro-1H-benzo[c]azepine-4,2-diyl))bis(2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanamide)
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C48H58N8O8
 1
1
Kd = 18.2 nM
   TI
   LI
   LO
   TS
CP0496996
(2S,2'S,2''S)-N,N',N''-((4S,4'S,4''S)-2,2',2''-(2,2',2''-(2,2',2''-nitrilotris(ethane-2,1-diyl)tris(azanediyl))tris(2-oxoethane-2,1-diyl))tris(3-oxo-2,3,4,5-tetrahydro-1H-benzo[c]azepine-4,2-diyl))tris(2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanamide)
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C75H93N13O12
 1
1
Kd = 22.91 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0000305
(-)-(etorphine)
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C17H19NO3
 2
1 Activity = 1220 nM
2 Ki = 684 nM
CP0040319
4-((R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-N,N-diethylbenzamide
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C27H37N3O2
 1
1 IC50 = 0.31 nM
CP0042565
(S)-3-((S)-2-{(R)-2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-N-{(S)-1-[(S)-1-(carbamoylmethyl-carbamoyl)-2-methyl-propylcarbamoyl]-2-methyl-propyl}-succinamic acid
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C37H52N8O10
 2
1 IC50 = 0.6 nM
2 Ki = 0.15 nM
CP0041255
(+)-4-((alpha R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-methoxyphenyl)methyl)-N,N-diethylbenzamide
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C28H39N3O2
 2
1 IC50 = 1.06 nM
2 Ki = 1.57 nM
CP0038418
13-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-1,2-dithia-5,8,11-triaza-cyclotetradecane-4-carboxylic acid
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C30H39N5O7S2
 4
1 IC50 = 1.6 nM
2 IC50 = 5.83 nM
3 IC50 = 8.5 nM
4 Ki = 2.72 nM
CP0050068
(1S,2S,13R,21R)-22-(cyclopropylmethyl)-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15,17,19(25)-heptaene-2,16-diol
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C26H26N2O3
 3
1 Ki = 0.062 nM
2 Ki = 0.22 nM
3 Ki = 0.41 nM
CP0167293
7-Benzylidenenaltrexone
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C27H27NO4
 1
1 Ki = 0.1 nM
CP0268775
(S)-4-((S)-2-{(R)-2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-4-{(1S,2S)-1-[(1S,2S)-1-(carbamoylmethyl-carbamoyl)-2-methyl-butylcarbamoyl]-2-methyl-butylcarbamoyl}-butyric acid
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C40H58N8O10
 1
1 Ki = 0.535 nM
CP0088373
(S)-2-[(S)-2-(2-{2-[(S)-2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-acetylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid
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C28H37N5O7
 2
1 Ki = 1.5 nM
2 Ki = 2.53 nM
CP0043301
(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]-N-methylacetamido}-N-(2-hydroxyethyl)-3-phenylpropanamide
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C26H35N5O6
 1
1 Ki = 2670 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00642 Opioid receptor, delta 1b Danio rerio, Zebrafish, Brachydanio rerio