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TargetKappa-type opioid receptor [D138A]
LigandBDBM21130
Substrate/Competitorn/a
Meas. Tech.Homologous Competition Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 2.9e+3±3e+2 nM
Commentsextracted
Citation Vardy, EMosier, PDFrankowski, KJWu, HKatritch, VWestkaemper, RBAubé, JStevens, RCRoth, BL Chemotype-selective modes of action of ¿-opioid receptor agonists. J Biol Chem288:34470-83 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Kappa-type opioid receptor [D138A]
Name:Kappa-type opioid receptor [D138A]
Synonyms:Kappa opioid receptor (KOR D138A) | OPRK | OPRK1 | OPRK_HUMAN
Type:Protein
Mol. Mass.:42605.76
Organism:Homo sapiens (Human)
Description:Human KOR with D138A mutation
Residue:380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIAYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM21130
n/a
NameBDBM21130
Synonyms:N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-yl]acetamide | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(4,5)dec-8-yl)benzeneacetamide | U-69593 | U69,593 | [3H]U69593
Typeradiolabeled ligand
Emp. Form.C22H32N2O2
Mol. Mass.356.5017
SMILESCN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N1CCCC1)C(=O)Cc1ccccc1
Structure
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