Reaction Details
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Kappa-type opioid receptor
Ligand
BDBM50493818
Substrate
n/a
Meas. Tech.
ChEMBL_989746 (CHEMBL2445984)
EC50
1400±n/a nM
Citation
Chen, XT; Pitis, P; Liu, G; Yuan, C; Gotchev, D; Cowan, CL; Rominger, DH; Koblish, M; Dewire, SM; Crombie, AL; Violin, JD; Yamashita, DS Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. J Med Chem 56:8019-31 (2013) [PubMed] Article More Info.:
Target
Name:
Kappa-type opioid receptor
Synonyms:
K-OR-1 | KOR-1 | Kappa-opioid receptor (KOR) | Kappa-type opioid receptor (KOPR) | Kappa-type opioid receptor (KOR) | Kappa-type opioid receptor (Kappa) | OPIATE Kappa | kappa opioid receptor (KOR) | OPRK_HUMAN | OPRK1 | OPRK
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
42648.76
Organism:
Human
Description:
P41145
Residue:
380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPVIITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYLMNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINICIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVLIIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALGSTSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRVRNTVQDPAYLRDIDGMNKPV
