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Assay Detail

CHEMBL4385883

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

Binding
Displacement of [3H]-U69593 from kappa-type opioid receptor in guinea pig brain membranes preincubated for 15 mins followed by [3H]-U69593 addition and measured after 90 mins by liquid scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membranes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.
Henry SP, Fernandez TJ, Anand JP, Griggs NW, Traynor JR, Mosberg HI.
J Med Chem (2019) 62 : 4142 -4157
PubMed 30924650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.17 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322568 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322568 Ki = 68.0 nM 7.17