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Assay Detail

CHEMBL3227799

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

Binding
Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO cells after 1 hr
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
Yuan Y, Arnatt CK, El-Hage N, Dever SM, Jacob JC, Selley DE, Hauser KF, Zhang Y.
Medchemcomm (2013) 4 : 847 -851
PubMed 23682308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.16 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 9.15
CHEMBL3219778 1 8.04
CHEMBL3219777 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE Ki = 0.7 nM 9.15
CHEMBL3219778 Ki = 9.2 nM 8.04
CHEMBL3219777 Ki = 51.8 nM 7.29