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Assay Detail

CHEMBL752954

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Binding
Binding affinity was evaluated by measuring the ability to displace [3H]DAMGO radioligand binding from Opioid receptor mu 1 in guinea pig brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 4 8.21 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317269 1 8.85
CHEMBL105665 1 8.21
CHEMBL317030 1 8.14
CHEMBL322796 CYPRODIME 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317269 Ki = 1.42 nM 8.85
CHEMBL105665 Ki = 6.15 nM 8.21
CHEMBL317030 Ki = 7.29 nM 8.14
CHEMBL322796 CYPRODIME Ki = 23.7 nM 7.62