Reaction Details |
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Target | Delta-type/Kappa-type/Mu-type opioid receptor |
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Ligand | BDBM50367061 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1354145 (CHEMBL3280909) |
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IC50 | 2.0±n/a nM |
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Citation | DeGraw, JI; Lawson, JA; Crase, JL; Johnson, HL; Ellis, M; Uyeno, ET; Loew, GH; Berkowitz, DS Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines. J Med Chem21:415-22 (1978) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Delta-type/Kappa-type/Mu-type opioid receptor |
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Name: | Delta-type/Kappa-type/Mu-type opioid receptor |
Synonyms: | Opioid receptor |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 1935286 |
Components: | This complex has 3 components. |
Component 1 |
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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Component 2 |
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 3 |
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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BDBM50367061 |
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n/a |
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Name | BDBM50367061 |
Synonyms: | NALORPHINE | NALORPHINE HYDROCHLORIDE |
Type | Small organic molecule |
Emp. Form. | C19H21NO3 |
Mol. Mass. | 311.3749 |
SMILES | O[C@H]1C=C[C@H]2[C@H]3Cc4ccc(O)c5O[C@@H]1[C@]2(CCN3CC=C)c45 |r,c:2,TLB:3:4:22.7.6:18.16.17| |
Structure |
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