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Assay Detail

CHEMBL2060903

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in mouse cerebellum
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
Nagase H, Imaide S, Hirayama S, Nemoto T, Fujii H.
Bioorg Med Chem Lett (2012) 22 : 5071 -5074
PubMed 22742909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.97 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2057693 1 9.37
CHEMBL483566 1 9.29
CHEMBL490665 NALFURAFINE HYDROCHLORIDE 4.0 1 9.23
CHEMBL2057692 1 7.61
CHEMBL2057691 1 7.08
CHEMBL485583 1 6.77
CHEMBL2057689 1 6.41
CHEMBL2057688 1 -
CHEMBL2057690 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2057693 Ki = 0.43 nM 9.37
CHEMBL483566 Ki = 0.51 nM 9.29
CHEMBL490665 NALFURAFINE HYDROCHLORIDE Ki = 0.582 nM 9.23
CHEMBL2057692 Ki = 24.6 nM 7.61
CHEMBL2057691 Ki = 83.2 nM 7.08
CHEMBL485583 Ki = 169.0 nM 6.77
CHEMBL2057689 Ki = 391.0 nM 6.41
CHEMBL2057688 Ki > 100000.0 nM -
CHEMBL2057690 Ki > 1000.0 nM -