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Assay Detail

CHEMBL1932292

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

Binding
Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig cerebrum membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists.
Ida Y, Nemoto T, Hirayama S, Fujii H, Osa Y, Imai M, Nakamura T, Kanemasa T, Kato A, Nagase H.
Bioorg Med Chem (2012) 20 : 949 -961
PubMed 22197670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.58 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559518 1 9.44
CHEMBL564538 1 8.36
CHEMBL552308 1 7.99
CHEMBL567175 NALTRINDOLE 1 7.85
CHEMBL1929363 1 7.83
CHEMBL1929365 1 7.76
CHEMBL1929364 1 6.58
CHEMBL1929362 1 6.29
CHEMBL327745 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559518 Ki = 0.36 nM 9.44
CHEMBL564538 Ki = 4.41 nM 8.36
CHEMBL552308 Ki = 10.2 nM 7.99
CHEMBL567175 NALTRINDOLE Ki = 14.0 nM 7.85
CHEMBL1929363 Ki = 14.8 nM 7.83
CHEMBL1929365 Ki = 17.5 nM 7.76
CHEMBL1929364 Ki = 263.4 nM 6.58
CHEMBL1929362 Ki = 516.2 nM 6.29
CHEMBL327745 Ki = 732.5 nM 6.13