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Assay Detail

CHEMBL1043333

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

Binding
Displacement of [3H]U69593 from guinea pig cerebellum kappa opioid receptor
4
Total Activities
4
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 Autocuration

Target

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

Publication

Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Nagase H, Watanabe A, Nemoto T, Yamaotsu N, Hayashida K, Nakajima M, Hasebe K, Nakao K, Mochizuki H, Hirono S, Fujii H.
Bioorg Med Chem Lett (2010) 20 : 121 -124
PubMed 19962305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.72 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2016680 1 9.96
CHEMBL1165548 1 9.82
CHEMBL485605 1 9.65
CHEMBL19019 NALTREXONE 4.0 1 9.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2016680 Ki = 0.111 nM 9.96
CHEMBL1165548 Ki = 0.152 nM 9.82
CHEMBL485605 Ki = 0.225 nM 9.65
CHEMBL19019 NALTREXONE Ki = 0.373 nM 9.43