Ki Summary

Reaction Details

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Target

Delta-type opioid receptor

Ligand

BDBM21132

Substrate/Competitor

BDBM21008

Meas. Tech.

Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay

7.4±n/a

Temperature

298.15±n/a K

2.2±n/a nM

EC50

120±n/a nM

Citation

Agnes, RS; Lee, YS; Davis, P; Ma, SW; Badghisi, H; Porreca, F; Lai, J; Hruby, VJ Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem49:2868-75 (2006) [PubMed] Article

More Info.:

Get all data from this article, Solution Info, Assay Method

Delta-type opioid receptor

Name:

Delta-type opioid receptor

Synonyms:

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

BDBM21132

BDBM21008

Name

BDBM21132

Synonyms:

(3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid | CCK-Opioid Peptide, 2 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2

Type

Peptide

Emp. Form.

C45H57N9O10

Mol. Mass.

883.9884

SMILES

CCCC[C@H](N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O

Structure