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Assay Detail

CHEMBL5133574

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

Binding
Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
Katoh K, Yamamoto N, Ishikawa Y, Irukayama-Tomobe Y, Tanimura R, Saitoh T, Nagumo Y, Kutsumura N, Yanagisawa M, Nagase H.
Bioorg Med Chem Lett (2022) 59 : 128527 -128527
PubMed 35007722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.13 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5185211 1 9.80
CHEMBL267495 NALFURAFINE 4.0 1 9.15
CHEMBL5188658 1 8.45
CHEMBL5204400 1 -
CHEMBL5181937 1 -
CHEMBL5186673 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5185211 Ki = 0.158 nM 9.80
CHEMBL267495 NALFURAFINE Ki = 0.7 nM 9.15
CHEMBL5188658 Ki = 3.57 nM 8.45
CHEMBL5204400 Ki > 5000.0 nM -
CHEMBL5181937 Ki > 10000.0 nM -
CHEMBL5186673 Ki > 10000.0 nM -