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Assay Detail

CHEMBL2020483

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

Binding
Displacement of [3H]DPDPE from kappa opioid receptor in guinea pig cerebellum membrane
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Watanabe Y, Kitazawa S, Fujii H, Nemoto T, Hirayama S, Nagase H.
Bioorg Med Chem Lett (2012) 22 : 2689 -2692
PubMed 22445285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 9.18 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2016678 1 9.72
CHEMBL2016675 1 9.54
CHEMBL2016676 1 9.47
CHEMBL2016679 1 9.46
CHEMBL2016672 1 9.33
CHEMBL2016673 1 9.07
CHEMBL2016674 1 8.85
CHEMBL2016677 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2016678 Ki = 0.19 nM 9.72
CHEMBL2016675 Ki = 0.29 nM 9.54
CHEMBL2016676 Ki = 0.34 nM 9.47
CHEMBL2016679 Ki = 0.35 nM 9.46
CHEMBL2016672 Ki = 0.47 nM 9.33
CHEMBL2016673 Ki = 0.86 nM 9.07
CHEMBL2016674 Ki = 1.42 nM 8.85
CHEMBL2016677 Ki = 9.91 nM 8.00