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Assay Detail

CHEMBL1027053

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

Binding
Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Nagase H, Osa Y, Nemoto T, Fujii H, Imai M, Nakamura T, Kanemasa T, Kato A, Gouda H, Hirono S.
Bioorg Med Chem Lett (2009) 19 : 2792 -2795
PubMed 19362480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.95 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
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 = 14.01 nM 7.85
CHEMBL327745 Ki = 732.45 nM 6.13