Reaction Details
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Kappa-type opioid receptor [Y139A]
Ligand
BDBM214798
Substrate
n/a
Meas. Tech.
cAMP Inhibition Assay
pH
7.4000±n/a
EC50
1.2e+2±1e+1 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 More Info.:
Target
Name:
Kappa-type opioid receptor [Y139A]
Synonyms:
OPRK_HUMAN | OPRK1 | OPRK | Kappa opioid receptor (KOR Y139A)
Type:
Protein
Mol. Mass.:
42556.66
Organism:
Human
Description:
Human KOR with Y139A mutation
Residue:
380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYLMNSWPFGDVLCKIVISIDAYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALGSTSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRVRNTVQDPAYLRDIDGMNKPV
Inhibitor
Name:
BDBM214798
Synonyms:
YGGFLRRIRPKLK | Dynorphin A (1-17)
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
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:
