Target
Delta-type opioid receptor
Ligand
BDBM21125
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
0.43±0.16 nM
EC50
0.83±0.05 nM
Citation
 Mollica, AGuardiani, GDavis, PMa, SWPorreca, FLai, JMannina, LSobolev, APHruby, VJ Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis. J Med Chem 50:3138-3142 (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:
BDBM21125
Synonyms:
(5S,8R,10Z,13R)-13-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]-5-benzyl-3,6,14-trioxo-1,4,7-triazacyclotetradec-10-ene-8-carboxylic acid | Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH | cDADAE(8)
Type:
Cyclic Peptide
Emp. Form.:
C28H33N5O7
Mol. Mass.:
551.5909
SMILES:
N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CC=CC[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O)C(O)=O |r,w:15.15|
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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