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Assay Detail

CHEMBL973311

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

Functional
Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50,488-stimulated [35S]GTPgammaS binding
4
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Wentland MP, Sun X, Cohen DJ, Bidlack JM.
Bioorg Med Chem (2008) 16 : 5653 -5664
PubMed 18417347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 2 - -
IC50 1 5.89 5.89
Imax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469189 2 5.89
CHEMBL493621 1 -
CHEMBL522375 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469189 IC50 = 1300.0 nM 5.89
CHEMBL493621 Activity - -
CHEMBL522375 Activity - -
CHEMBL469189 Imax = 75.0 % -