| Reaction Details |
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 | Report a problem with these data |
| Target | Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1 |
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| Ligand | BDBM50247803 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_146289 (CHEMBL873626) |
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| IC50 | 1.0±n/a nM |
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| Citation |  Schoenecker, JW; Takemori, AE; Portoghese, PS Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine. J Med Chem29:1868-71 (1986) [PubMed] |
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| More Info.: | Get all data from this article, Assay Method |
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| Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1 |
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| Name: | Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1 |
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| Synonyms: | Opioid receptor |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 172778 |
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| Components: | This complex has 4 components. |
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| Component 1 |
| Name: | Mu-type opioid receptor |
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| Synonyms: | MOR-1 | MUOR1 | Mu-type opioid receptor (MOR) | OPIATE Mu | OPRM_RAT | Opiate non-selective | Opioid receptor B | Oprm1 | Ror-b |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 44503.11 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Competition binding assays were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the mu opioid receptor. |
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| Residue: | 398 |
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| Sequence: | MDSSTGPGNTSDCSDPLAQASCSPAPGSWLNLSHVDGNQSDPCGLNRTGLGGNDSLCPQT
GSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATST
LPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRT
PRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFA
FIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYV
IIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQ
QNSTRVRQNTREHPSTANTVDRTNHQLENLEAETAPLP
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| Component 2 |
| Name: | Sigma non-opioid intracellular receptor 1 |
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| Synonyms: | Opioid receptor | Oprs1 | SGMR1_RAT | Sigma | Sigma non-opioid intracellular receptor 1 | Sigma opioid receptor | Sigma-1 | Sigmar1 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 25266.54 |
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| Organism: | RAT |
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| Description: | Q9R0C9 |
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| Residue: | 223 |
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| Sequence: | MPWAVGRRWAWITLFLTIVAVLIQAVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSR
LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSHGHSGRY
WAEISDTIISGTFHQWREGTTKSEVYYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPS
TLAFALSDTIFSTQDFLTLFYTLRAYARGLRLELTTYLFGQDP
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| Component 3 |
| Name: | Kappa-type opioid receptor |
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| Synonyms: | KOR-1 | Kappa Opioid Receptor | OPIATE Kappa | OPRK_RAT | Opioid receptor | Oprk1 | Ror-d |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 42692.90 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | P34975 |
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| Residue: | 380 |
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| Sequence: | MESPIQIFRGEPGPTCAPSACLLPNSSSWFPNWAESDSNGSVGSEDQQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSAVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLASSVGISAIVLGGTKVREDVDVIECSLQFPDDEYSWWDLFMKICVFVFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITKLVLVVVAVFIICWTPIHIFILVEALG
STSHSTAVLSSYYFCIALGYTNSSLNPVLYAFLDENFKRCFRDFCFPIKMRMERQSTNRV
RNTVQDPASMRDVGGMNKPV
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| Component 4 |
| Name: | Delta-type opioid receptor |
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| 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 |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 40465.04 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | Competition binding assays were using CHO-K1 cell membranes expressing the opioid receptor. |
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| Residue: | 372 |
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| Sequence: | MEPVPSARAELQFSLLANVSDTFPSAFPSASANASGSPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKLKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTQPRDGAVVCTLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDINRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRAPCGGQEPGSLRRPRQATARERVTAC
TPSDGPGGGAAA
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| BDBM50247803 |
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| n/a |
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| Name | BDBM50247803 |
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| Synonyms: | Beta-Funeltrexamine | CHEMBL473136 | beta-funaltrexamine | methyl (2E)-3-{[(1S,5R,13R,14R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-trien-14-yl]carbamoyl}prop-2-enoate | methyl 3-[4-cyclopropylmethyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-ylcarbamoyl]-(E)-2-propenoate |
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| Type | Small organic molecule |
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| Emp. Form. | C25H30N2O6 |
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| Mol. Mass. | 454.5155 |
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| SMILES | COC(=O)\C=C\C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5O[C@@H]1[C@]2(CCN3CC1CC1)c45 |r| |
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| Structure | 
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