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TargetDelta-type opioid receptor
LigandBDBM21020
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 5.0±n/a nM
EC50 9.6±n/a nM
Citation Yamamoto, TNair, PDavis, PMa, SWNavratilova, EMoye, STumati, SLai, JVanderah, TWYamamura, HIPorreca, FHruby, VJ Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists. J Med Chem50:2779-86 (2007) [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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BDBM21020
BDBM21008
NameBDBM21020
Synonyms:Bifunctional Peptide Ligand, 4 (TY004) | H-Tyr-D-Ala-Gly-Phe-Leu-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanamido]-4-methylpentanoyl]pyrrolidin-2-yl]formamido}-4-methylpentanamido]-3-(1H-indol-3-yl)propanoate
TypePeptide-like ligand
Emp. Form.C60H71F6N9O10
Mol. Mass.1192.2505
SMILESCC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=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)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F
Structure
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