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Target
Kappa-type opioid receptor [I294A]
Ligand
BDBM21130
Substrate
n/a
Meas. Tech.
cAMP Inhibition Assay
pH
7.4000±n/a
EC50
4.7±0.9 nM
Comments
extracted
Citation
 Vardy, E; Mosier, PD; Frankowski, KJ; Wu, H; Katritch, V; Westkaemper, RB; Aubé, J; Stevens, RC; Roth, 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 [I294A]
Synonyms:
OPRK_HUMAN | OPRK1 | OPRK | Kappa opioid receptor (KOR I294A)
Type:
Protein
Mol. Mass.:
42606.68
Organism:
Human
Description:
Human KOR with I294A mutation
Residue:
380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYLMNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFALVEALGSTSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRVRNTVQDPAYLRDIDGMNKPV
  
Inhibitor
Name:
BDBM21130
Synonyms:
U69,593 | N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(4,5)dec-8-yl)benzeneacetamide | U-69593 | N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-yl]acetamide | [3H]U69593
Type:
radiolabeled ligand
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity: