Reaction Details |
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Target | Delta-type opioid receptor |
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Ligand | BDBM21011 |
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Substrate/Competitor | BDBM21008 |
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Meas. Tech. | Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay |
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pH | 7.4±n/a |
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Temperature | 298.15±n/a K |
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Ki | 77±n/a nM |
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EC50 | 150±n/a nM |
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Citation | Yamamoto, T; Nair, P; Vagner, J; Largent-Milnes, T; Davis, P; Ma, SW; Navratilova, E; Moye, S; Tumati, S; Lai, J; Yamamura, HI; Vanderah, TW; Porreca, F; Hruby, 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 |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Delta-type opioid receptor |
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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 |
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BDBM21008 |
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Name | BDBM21011 |
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 |
Type | Peptide-like ligand |
Emp. Form. | C53H65N9O8 |
Mol. Mass. | 956.1387 |
SMILES | CC(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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