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Assay Detail

CHEMBL754204

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Binding
Binding affinity determined by displacing [3H]DAMGO from Opioid receptor mu 1 in rat brain membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Brain membranes
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
Spetea M, Schüllner F, Moisa RC, Berzetei-Gurske IP, Schraml B, Dörfler C, Aceto MD, Harris LS, Coop A, Schmidhammer H.
J Med Chem (2004) 47 : 3242 -3247
PubMed 15163203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.18 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110640 1 6.47
CHEMBL325347 1 6.40
CHEMBL321170 1 6.08
CHEMBL322796 CYPRODIME 1 4.97
CHEMBL109741 1 4.94
CHEMBL326860 1 4.86
CHEMBL109441 1 4.83
CHEMBL109786 1 4.55
CHEMBL409832 1 4.36
CHEMBL322738 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110640 Ki = 340.0 nM 6.47
CHEMBL325347 Ki = 400.0 nM 6.40
CHEMBL321170 Ki = 840.0 nM 6.08
CHEMBL322796 CYPRODIME Ki = 10600.0 nM 4.97
CHEMBL109741 Ki = 11600.0 nM 4.94
CHEMBL326860 Ki = 13800.0 nM 4.86
CHEMBL109441 Ki = 14900.0 nM 4.83
CHEMBL109786 Ki = 27900.0 nM 4.55
CHEMBL409832 Ki = 43300.0 nM 4.36
CHEMBL322738 Ki = 44900.0 nM 4.35