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Assay Detail

CHEMBL872675

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

Binding
In vitro binding affinity at opioid receptor kappa 1 was determined in human CHO cells using [3H]U-69593
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

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 8.69 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL606986 1 10.10
CHEMBL606925 1 9.96
CHEMBL606985 1 9.43
CHEMBL514774 1 9.39
CHEMBL606924 1 9.31
CHEMBL606987 1 9.22
CHEMBL606923 1 8.85
CHEMBL606876 1 7.21
CHEMBL70 MORPHINE 4.0 1 6.95
CHEMBL326684 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL606986 Ki = 0.08 nM 10.10
CHEMBL606925 Ki = 0.11 nM 9.96
CHEMBL606985 Ki = 0.37 nM 9.43
CHEMBL514774 Ki = 0.41 nM 9.39
CHEMBL606924 Ki = 0.49 nM 9.31
CHEMBL606987 Ki = 0.6 nM 9.22
CHEMBL606923 Ki = 1.4 nM 8.85
CHEMBL606876 Ki = 61.4 nM 7.21
CHEMBL70 MORPHINE Ki = 113.0 nM 6.95
CHEMBL326684 Ki = 304.0 nM 6.52