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Assay Detail

CHEMBL756033

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Binding
The opioid receptor affinity(Ki) was evaluated by competition with [3H]-DPDPE (delta 1) on guinea pig brain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice.
Portoghese PS, Farouz-Grant F, Sultana M, Takemori AE.
J Med Chem (1995) 38 : 402 -407
PubMed 7853332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 10.05 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132420 1 10.89
CHEMBL567175 NALTRINDOLE 1 10.52
CHEMBL334970 1 9.85
CHEMBL334715 1 9.80
CHEMBL132897 1 9.74
CHEMBL335936 1 9.52
CHEMBL422258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132420 Ki = 0.013 nM 10.89
CHEMBL567175 NALTRINDOLE Ki = 0.03 nM 10.52
CHEMBL334970 Ki = 0.14 nM 9.85
CHEMBL334715 Ki = 0.16 nM 9.80
CHEMBL132897 Ki = 0.18 nM 9.74
CHEMBL335936 Ki = 0.3 nM 9.52
CHEMBL422258 Ki = 0.005 nM -