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TargetDelta-type opioid receptor
LigandBDBM21011
Substrate/CompetitorBDBM21008
Meas. Tech.Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 77±n/a nM
EC50 150±n/a nM
Citation Yamamoto, TNair, PVagner, JLargent-Milnes, TDavis, PMa, SWNavratilova, EMoye, STumati, SLai, JYamamura, HIVanderah, TWPorreca, FHruby, VJ A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists. J Med Chem51:1369-76 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Delta-type opioid receptor
Name:Delta-type opioid receptor
Synonyms:D-OR-1 | DOR-1 | Delta opioid receptor | Delta-type opioid receptor (Delta) | OPIATE Delta | OPRD | OPRD1 | OPRD_HUMAN | OPRK1 | opioid receptor, delta 1
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:40382.98
Organism:Homo sapiens (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:
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC
TPSDGPGGGAAA
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BDBM21011
BDBM21008
NameBDBM21011
Synonyms:(2S)-2-{[(2S)-1-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-1-[benzyl(methyl)carbamoyl]-2-(1H-indol-3-yl)ethyl]-4-methylpentanamide | C-terminal modified bifunctional peptide, 4 | H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl
TypePeptide-like ligand
Emp. Form.C53H65N9O8
Mol. Mass.956.1387
SMILESCC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)Cc1ccccc1
Structure
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