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Assay Detail

CHEMBL755200

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Binding
In vivo binding affinity was evaluated by measuring the ability to displace [3H]DPDPE radioligand binding from delta opioid receptor in guinea pig brain membranes
6
Total Activities
6
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

Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime.
Schmidhammer H, Jennewein HK, Krassnig R, Traynor JR, Patel D, Bell K, Froschauer G, Mattersberger K, Jachs-Ewinger C, Jura P.
J Med Chem (1995) 38 : 3071 -3077
PubMed 7636870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.37 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105665 1 7.86
CHEMBL317269 1 7.67
CHEMBL317030 1 7.59
CHEMBL322195 1 7.38
CHEMBL322796 CYPRODIME 1 7.21
CHEMBL104310 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105665 Ki = 13.8 nM 7.86
CHEMBL317269 Ki = 21.4 nM 7.67
CHEMBL317030 Ki = 25.6 nM 7.59
CHEMBL322195 Ki = 42.0 nM 7.38
CHEMBL322796 CYPRODIME Ki = 61.1 nM 7.21
CHEMBL104310 Ki = 334.0 nM 6.48