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Target
Delta-type opioid receptor
Ligand
BDBM21014
Substrate
BDBM21008
Meas. Tech.
Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
2.6±n/a nM
EC50
1.1±n/a nM
Citation
 Yamamoto, T; Nair, P; Davis, P; Ma, SW; Navratilova, E; Moye, S; Tumati, S; Lai, J; Vanderah, TW; Yamamura, HI; Porreca, F; Hruby, 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 Chem 50:2779-86 (2007) [PubMed]  Article 
Target
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:
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVCAVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELLCKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVGVPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRLRSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAALHLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTACTPSDGPGGGAAA
  
Inhibitor
Name:
BDBM21014
Synonyms:
(2S)-2-amino-N-[(1R)-1-[({[(1S)-1-{N'-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]hydrazinecarbonyl}-2-phenylethyl]carbamoyl}methyl)carbamoyl]ethyl]-3-(4-hydroxyphenyl)propanamide | (Tyr-Ala-Gly-Phe-NH2)2 | Biphalin | CHEMBL200199 | bis(Tyr-Ala-Gly-PheNH2)hydrazide | enkephalin dimer
Type:
Analgesics
Emp. Form.:
C46H56N10O10
Mol. Mass.:
908.9978
SMILES:
C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
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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