Target
Kappa-type opioid receptor [H291A]
Ligand
BDBM21130
Substrate
n/a
Meas. Tech.
cAMP Inhibition Assay
pH
7.4±n/a
EC50
1.3e+2±2e+1 nM
Comments
extracted
Citation
 Vardy, EMosier, PDFrankowski, KJWu, HKatritch, VWestkaemper, RBAubé, JStevens, RCRoth, BL Chemotype-selective modes of action of ¿-opioid receptor agonists. J Biol Chem 288:34470-83 (2013) [PubMed]  Article 
Target
Name:
Kappa-type opioid receptor [H291A]
Synonyms:
Kappa opioid receptor (KOR H291A) | OPRK | OPRK1 | OPRK_HUMAN
Type:
Protein
Mol. Mass.:
42582.19
Organism:
Homo sapiens (Human)
Description:
Human KOR with H291A mutation
Residue:
380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYLMNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIAIFILVEALGSTSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRVRNTVQDPAYLRDIDGMNKPV
  
Inhibitor
Name:
BDBM21130
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
Type:
radiolabeled ligand
Emp. Form.:
C22H32N2O2
Mol. Mass.:
356.5017
SMILES:
CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N1CCCC1)C(=O)Cc1ccccc1
Structure:
Search PDB for entries with ligand similarity: