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Target
Delta-type opioid receptor/Kappa-type opioid receptor/Mu-type opioid receptor/Sigma non-opioid intracellular receptor 1
Ligand
BDBM50228260
Substrate
n/a
Meas. Tech.
ChEMBL_147659 (CHEMBL756574)
Ki
8.2±n/a nM
Citation
 Colapret, JA; Diamantidis, G; Spencer, HK; Spaulding, TC; Rudo, FG Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines. J Med Chem 32:968-74 (1989) [PubMed]  Article 
Target
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:
MDSSTGPGNTSDCSDPLAQASCSPAPGSWLNLSHVDGNQSDPCGLNRTGLGGNDSLCPQTGSPSMVTAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATSTLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRTPRNAKIVNVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYVIIKALITIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSTIEQQNSTRVRQNTREHPSTANTVDRTNHQLENLEAETAPLP
  
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:
MPWAVGRRWAWITLFLTIVAVLIQAVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSRLIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSHGHSGRYWAEISDTIISGTFHQWREGTTKSEVYYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPSTLAFALSDTIFSTQDFLTLFYTLRAYARGLRLELTTYLFGQDP
  
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:
MESPIQIFRGEPGPTCAPSACLLPNSSSWFPNWAESDSNGSVGSEDQQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSAVYLMNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLASSVGISAIVLGGTKVREDVDVIECSLQFPDDEYSWWDLFMKICVFVFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITKLVLVVVAVFIICWTPIHIFILVEALGSTSHSTAVLSSYYFCIALGYTNSSLNPVLYAFLDENFKRCFRDFCFPIKMRMERQSTNRVRNTVQDPASMRDVGGMNKPV
  
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:
MEPVPSARAELQFSLLANVSDTFPSAFPSASANASGSPGARSASSLALAIAITALYSAVCAVGLLGNVLVMFGIVRYTKLKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTQPRDGAVVCTLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDINRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRAPCGGQEPGSLRRPRQATARERVTACTPSDGPGGGAAA
  
Inhibitor
Name:
BDBM50228260
Synonyms:
CHEMBL367286
Type:
Small organic molecule
Emp. Form.:
C26H36N2O3S
Mol. Mass.:
456.641
SMILES:
CCCC(=O)OCC1(CCN(CCc2cccs2)CC1)N(C(=O)CCC)c1ccccc1
Structure:
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