Target
Kappa-type opioid receptor [Y312A]
Ligand
BDBM214799
Substrate
n/a
Meas. Tech.
Homologous Competition Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
3.9e+2±1.7e+2 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 [Y312A]
Synonyms:
Kappa opioid receptor (KOR Y312A) | OPRK | OPRK1 | OPRK_HUMAN
Type:
Protein
Mol. Mass.:
42556.66
Organism:
Homo sapiens (Human)
Description:
Human KOR with Y312A mutation
Residue:
380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYLMNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALGSTSHSTAALSSAYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRVRNTVQDPAYLRDIDGMNKPV
  
Inhibitor
Name:
BDBM214799
Synonyms:
1xx
Type:
Small organic molecule
Emp. Form.:
C24H22ClF3N2O2
Mol. Mass.:
462.892
SMILES:
FC(F)(F)c1cc(NC(=O)[C@H]2CC=C[C@H]3CCN(Cc4ccccc4)C(=O)[C@@H]23)ccc1Cl |r,c:12|
Structure:
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