Reaction Details
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Delta-type opioid receptor
Ligand
BDBM50493818
Substrate
n/a
Meas. Tech.
ChEMBL_989745 (CHEMBL2445983)
EC50
2800±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:
Delta-type opioid receptor
Synonyms:
D-OR-1 | DOR-1 | Delta opioid receptor | Delta-type opioid receptor (Delta) | OPIATE Delta | OPRK1 | opioid receptor, delta 1 | OPRD_HUMAN | OPRD1 | OPRD
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
40382.98
Organism:
Human
Description:
Competition binding assays were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the delta opioid receptor.
Residue:
372
Sequence:
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVCAVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTACTPSDGPGGGAAA
