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TargetOpioid receptors; mu/kappa/delta
LigandBDBM50001714
Substrate/Competitorn/a
Meas. Tech.ChEBML_145721
IC50 1.3±n/a nM
Citation Klein PNelson WL O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay. J Med Chem 35:4589-94 (1993) [PubMed]
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:Cannabinoid receptor 1/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:P41145
Residue:380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
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Component 3
Name:Delta-type opioid receptor
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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BDBM50001714
n/a
NameBDBM50001714
Synonyms:2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-(1S,2R,6S,14R,15R,16R)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-2-propanol | 2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-(1S,2R,6S,14R,15R,16R)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-2-propanol(diprenorphine) | 2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7(12),8,10-trien-16-yl]-2-propanol | CHEMBL281786 | DIPRENORPHINE-HCl | Diprenorphine
TypeSmall organic molecule
Emp. Form.C26H35NO4
Mol. Mass.425.5604
SMILESCO[C@]12CC[C@@]3(C[C@@H]1C(C)(C)O)[C@H]1Cc4ccc(O)c5O[C@@H]2[C@]3(CCN1CC1CC1)c45 |THB:8:7:22.21:4.3|
Structure
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