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TargetOpioid receptors; mu/kappa/delta
LigandBDBM50000788
Substrate/Competitorn/a
Meas. Tech.ChEMBL_145870
IC50 43±n/a nM
Citation Dasher, WEKlein, PNelson, WL Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol. J Med Chem35:2374-84 (1992) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Opioid receptors; mu/kappa/delta
Name:Opioid receptors; mu/kappa/delta
Synonyms:n/a
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 357797
Components:This complex has 3 components.
Component 1
Name:Mu-type opioid receptor
Synonyms:M-OR-1 | MOP | MOR-1 | MUOR1 | Mu Opioid Receptor | Mu opiate receptor | OPIATE Mu | OPRM1 | hMOP | mu-type opioid receptor isoform MOR-1
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:44789.51
Organism:Homo sapiens (Human)
Description:P35372
Residue:400
Sequence:
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
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Component 2
Name:Opioid receptors; mu/kappa/delta
Synonyms:K-OR-1 | KOR-1 | Kappa-opioid receptor (KOR) | Kappa-type opioid receptor (KOPR) | Kappa-type opioid receptor (KOR) | Kappa-type opioid receptor (Kappa) | OPIATE Kappa | OPRK | OPRK1 | kappa opioid receptor (KOR)
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:42648.76
Organism:Homo sapiens (Human)
Description:Competition binding assays were carried out using membrane preparations from HEK-293 cells stably expressing KOP receptors.
Residue:380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
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Component 3
Name:Opioid receptors; mu/kappa/delta
Synonyms:D-OR-1 | DOR-1 | Delta-type opioid receptor (Delta) | OPIATE Delta | OPRD | OPRD1 | OPRK1 | opioid receptor, delta 1
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:40382.98
Organism:Homo sapiens (Human)
Description:Competition binding assays were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the delta opioid receptor.
Residue:372
Sequence:
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC
TPSDGPGGGAAA
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BDBM50000788
NameBDBM50000788
Synonyms:(morphine)4-methyl-(1S,5R,13R,14S,17R)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10,15-tetraene-10,14-diol | (naloxone) 4-allyl-10,17-dihydroxy-(1S,5R,13R,17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one | (naloxone)4-allyl-10,17-dihydroxy-(1S,5R,13R,17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one | (naloxone)4-allyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one | 4-allyl-10,17-dihydroxy-(1S,5R,13R,17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one | 4-allyl-10,17-dihydroxy-(1S,5R,13R,17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one (naloxone) | 4-allyl-10,17-dihydroxy-(1S,5R,13R,17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one( Naloxone) | 4-allyl-10,17-dihydroxy-(1S,5R,13R,17S)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one(Naxolone) | 4-allyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one | 4-allyl-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10-trien-14-one(naloxone)C2H2O4 | Analog of 14-(Arylhydroxyamino)codeinone | NALOXONE | NARCAN | SUBOXONE | [17-(2,3-3H-2-propenyl)]-4, 5a -epoxy-3,14-dihydroxymorphinan-6-one
TypeSmall organic molecule
Emp. Form.C19H21NO4
Mol. Mass.327.3743
SMILESOc1ccc2C[C@H]3N(CC=C)CC[C@@]45[C@@H](Oc1c24)C(=O)CC[C@@]35O |r|
Structure
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n/a