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TargetDelta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1
LigandBDBM50225687
Substrate/Competitorn/a
Meas. Tech.ChEMBL_146285 (CHEMBL756530)
IC50 4.0±n/a nM
Citation Koolpe, GANelson, WLGioannini, TLAngel, LAppelmans, NSimon, EJ Opioid agonists and antagonists. 6-Desoxy-6-substituted lactone, epoxide, and glycidate ester derivatives of naltrexone and oxymorphone. J Med Chem28:949-57 (1985) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1
Name:Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1
Synonyms:Opioid receptor
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 172778
Components:This complex has 4 components.
Component 1
Name:Mu-type opioid receptor
Synonyms:MOR-1 | MUOR1 | Mu-type opioid receptor (MOR) | OPIATE Mu | OPRM_RAT | Opiate non-selective | Opioid receptor B | Oprm1 | Ror-b
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:44503.11
Organism:Rattus norvegicus (rat)
Description:Competition binding assays were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the mu opioid receptor.
Residue:398
Sequence:
MDSSTGPGNTSDCSDPLAQASCSPAPGSWLNLSHVDGNQSDPCGLNRTGLGGNDSLCPQT
GSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATST
LPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRT
PRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFA
FIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYV
IIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQ
QNSTRVRQNTREHPSTANTVDRTNHQLENLEAETAPLP
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Component 2
Name:Sigma non-opioid intracellular receptor 1
Synonyms:Opioid receptor | Oprs1 | SGMR1_RAT | Sigma | Sigma non-opioid intracellular receptor 1 | Sigma opioid receptor | Sigma-1 | Sigmar1
Type:Enzyme Catalytic Domain
Mol. Mass.:25266.54
Organism:RAT
Description:Q9R0C9
Residue:223
Sequence:
MPWAVGRRWAWITLFLTIVAVLIQAVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSR
LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSHGHSGRY
WAEISDTIISGTFHQWREGTTKSEVYYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPS
TLAFALSDTIFSTQDFLTLFYTLRAYARGLRLELTTYLFGQDP
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Component 3
Name:Kappa-type opioid receptor
Synonyms:KOR-1 | Kappa Opioid Receptor | OPIATE Kappa | OPRK_RAT | Opioid receptor | Oprk1 | Ror-d
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:42692.90
Organism:Rattus norvegicus (rat)
Description:P34975
Residue:380
Sequence:
MESPIQIFRGEPGPTCAPSACLLPNSSSWFPNWAESDSNGSVGSEDQQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSAVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLASSVGISAIVLGGTKVREDVDVIECSLQFPDDEYSWWDLFMKICVFVFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITKLVLVVVAVFIICWTPIHIFILVEALG
STSHSTAVLSSYYFCIALGYTNSSLNPVLYAFLDENFKRCFRDFCFPIKMRMERQSTNRV
RNTVQDPASMRDVGGMNKPV
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Component 4
Name:Delta-type opioid receptor
Synonyms:Cytochrome P450 3A4 | DOR-1 | Delta opioid receptor | Delta-type opioid receptor | Delta-type opioid receptor (DOR) | OPIATE Delta | OPRD_RAT | Opiate Delta 1 | Opioid receptor | Opioid receptor A | Opioid receptors; mu & delta | Oprd1 | Ror-a | Voltage-gated potassium channel
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:40465.04
Organism:Rattus norvegicus (rat)
Description:Competition binding assays were using CHO-K1 cell membranes expressing the opioid receptor.
Residue:372
Sequence:
MEPVPSARAELQFSLLANVSDTFPSAFPSASANASGSPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKLKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTQPRDGAVVCTLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDINRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRAPCGGQEPGSLRRPRQATARERVTAC
TPSDGPGGGAAA
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BDBM50225687
n/a
NameBDBM50225687
Synonyms:CHEMBL611128
TypeSmall organic molecule
Emp. Form.C21H25NO4
Mol. Mass.355.4275
SMILES[H][C@@]12Cc3ccc(O)c4OC5C6(CO6)CCC1(O)[C@@]5(CCN2CC1CC1)c34 |r,THB:22:21:16:26.3.2|
Structure
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