Target
Kappa-type opioid receptor [Y139F]
Ligand
BDBM214798
Substrate
n/a
Meas. Tech.
Homologous Competition Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
29±11 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 [Y139F]
Synonyms:
Kappa opioid receptor (KOR Y139F) | OPRK | OPRK1 | OPRK_HUMAN
Type:
Protein
Mol. Mass.:
42632.76
Organism:
Homo sapiens (Human)
Description:
Human KOR with Y139F mutation
Residue:
380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYLMNSWPFGDVLCKIVISIDFYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALGSTSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRVRNTVQDPAYLRDIDGMNKPV
  
Inhibitor
Name:
BDBM214798
Synonyms:
Dynorphin A (1-17) | YGGFLRRIRPKLK
Type:
Small organic molecule
Emp. Form.:
C75H126N24O15
Mol. Mass.:
1603.9547
SMILES:
CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(O)=O |r|
Structure:
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