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Assay Detail

CHEMBL750071

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

Binding
Displacement of radioligand [3H]- U-69,593 on Opioid receptor kappa 1 in monkey brain membranes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.
Derrick I, Neilan CL, Andes J, Husbands SM, Woods JH, Traynor JR, Lewis JW.
J Med Chem (2000) 43 : 3348 -3350
PubMed 10966754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.84 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386492 CLOCINNAMOX 1 8.14
CHEMBL386272 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386492 CLOCINNAMOX Ki = 7.2 nM 8.14
CHEMBL386272 Ki = 29.0 nM 7.54