Reaction Details Report a problem with these data
Target
Delta-type opioid receptor
Ligand
BDBM21007
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
50±n/a nM
EC50
35±n/a nM
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 Chem 51:1369-76 (2008) [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:
BDBM21007
Synonyms:
C-terminal modified bifunctional peptide, 1 | H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 | [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-4-methylpentanamido]-3-(1H-indol-3-yl)propanoate
Type:
Peptide-like ligand
Emp. Form.:
C54H60F6N8O9
Mol. Mass.:
1079.0928
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)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F
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:
Search PDB for entries with ligand similarity: