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Assay Detail

CHEMBL753670

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
Anzini M, Canullo L, Braile C, Cappelli A, Gallelli A, Vomero S, Menziani MC, De Benedetti PG, Rizzo M, Collina S, Azzolina O, Sbacchi M, Ghelardini C, Galeotti N.
J Med Chem (2003) 46 : 3853 -3864
PubMed 12930147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.74 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567175 NALTRINDOLE 1 9.80
CHEMBL127828 1 7.82
CHEMBL127969 1 6.98
CHEMBL70 MORPHINE 4.0 1 6.34
CHEMBL124015 1 -
CHEMBL440765 U-69593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567175 NALTRINDOLE Ki = 0.16 nM 9.80
CHEMBL127828 Ki = 15.3 nM 7.82
CHEMBL127969 Ki = 105.0 nM 6.98
CHEMBL70 MORPHINE Ki = 456.0 nM 6.34
CHEMBL124015 Ki > 1000.0 nM -
CHEMBL440765 U-69593 Ki > 10000.0 nM -