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Assay Detail

CHEMBL5127637

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

Binding
Displacement of [3H]U69593 from guinea pig brain membrane KOP incubated for 1 hr by scintillation counter analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
Smith MT, Kong D, Kuo A, Imam MZ, Williams CM.
J Med Chem (2022) 65 : 1612 -1661
PubMed 34995453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.41 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2396991 1 7.75
CHEMBL5178271 1 7.54
CHEMBL5187788 1 7.26
CHEMBL5178409 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2396991 Ki = 18.0 nM 7.75
CHEMBL5178271 Ki = 29.0 nM 7.54
CHEMBL5187788 Ki = 55.0 nM 7.26
CHEMBL5178409 Ki = 85.0 nM 7.07