Reaction Details |
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Target | Delta-type opioid receptor |
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Ligand | BDBM21008 |
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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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Kd | 0.45±0.1 nM |
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EC50 | 1.6±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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BDBM21008 |
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BDBM21008 |
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Name | BDBM21008 |
Synonyms: | (4S,7S,13S)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-7-benzyl-3,3,14,14-tetramethyl-6,9,12-trioxo-1,2-dithia-5,8,11-triazacyclotetradecane-4-carboxylic acid | CHEMBL31421 | DPDPE | DPDPE-Cl | DPDPE-OH | Enkephalin, [Tyrosyl-2,6-3H(N)]- (2-D-Penicillamine, 5-D-Penicillamine) | [3H]DPDPE |
Type | Analgesics |
Emp. Form. | C30H39N5O7S2 |
Mol. Mass. | 645.79 |
SMILES | CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]1C(O)=O |
Structure |
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