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Assay Detail

CHEMBL758580

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Binding
In vitro binding affinity at opioid receptor mu 1 was determined in C6 rat glioma cells using [3H]DAMGO
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C6
Confidence 8 — Homologous 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. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.
Greiner E, Spetea M, Krassnig R, Schüllner F, Aceto M, Harris LS, Traynor JR, Woods JH, Coop A, Schmidhammer H.
J Med Chem (2003) 46 : 1758 -1763
PubMed 12699394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 9.34 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL326684 1 10.64
CHEMBL606985 1 10.05
CHEMBL606925 1 9.70
CHEMBL606986 1 9.70
CHEMBL606924 1 9.60
CHEMBL514774 1 9.47
CHEMBL606987 1 8.96
CHEMBL606923 1 8.72
CHEMBL606876 1 8.42
CHEMBL70 MORPHINE 4.0 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL326684 Ki = 0.023 nM 10.64
CHEMBL606985 Ki = 0.09 nM 10.05
CHEMBL606925 Ki = 0.2 nM 9.70
CHEMBL606986 Ki = 0.2 nM 9.70
CHEMBL606924 Ki = 0.25 nM 9.60
CHEMBL514774 Ki = 0.34 nM 9.47
CHEMBL606987 Ki = 1.1 nM 8.96
CHEMBL606923 Ki = 1.9 nM 8.72
CHEMBL606876 Ki = 3.8 nM 8.42
CHEMBL70 MORPHINE Ki = 6.55 nM 8.18